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Adriaan IJzerman

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TOP 3
Tom De Bruyn; Peter De Witte; Adriaan P IJzerman; Bruno Stieger; Gerard J P van Westen; Patrick F Augustijns; Pieter Annaert
Structure-Based Identification of OATP1B1/3 Inhibitors.
João F S Carvalho; Maarten L J Doornbos; Elisabeth Klaasse; Julien Louvel; Zhiyi Yu; Johannes Brussee; Adriaan P IJzerman
Strategies to reduce HERG k(+) channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Dong Guo; Johannes Brussee; Adriaan P IJzerman; Thea Mulder-Krieger; Erika J H van Dorp; Jacobus P D van Veldhoven; Laura Heitman
Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics.

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2013: Tom De Bruyn; Peter De Witte; Adriaan P IJzerman; Bruno Stieger; Gerard J P van Westen; Patrick F Augustijns; Pieter Annaert
Structure-Based Identification of OATP1B1/3 Inhibitors.
Molecular pharmacology 2013;83(6):1257-67.
2013: João F S Carvalho; Maarten L J Doornbos; Elisabeth Klaasse; Julien Louvel; Zhiyi Yu; Johannes Brussee; Adriaan P IJzerman
Strategies to reduce HERG k(+) channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Journal of medicinal chemistry 2013;56(7):2828-40.
2013: Dong Guo; Johannes Brussee; Adriaan P IJzerman; Thea Mulder-Krieger; Erika J H van Dorp; Jacobus P D van Veldhoven; Laura Heitman
Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics.
Journal of biomolecular screening 2013;18(3):309-20.
2013: Gerard J P van Westen; Jörg K Wegner; Alwin Hendriks; Adriaan P IJzerman; Herman van Vlijmen; Andreas Bender
Significantly improved HIV inhibitor efficacy prediction employing proteochemometric models generated from antivirogram data.
PLoS computational biology 2013;9(2):e1002899.
2012: Dan Chen; James Errey; Laura H Heitman; Adriaan P IJzerman; Fiona H Marshall; Gregg Siegal
Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity.
ACS chemical biology 2012;7(12):2064-73.
2012: Zhaosha Li; Theo J C Van Berkel; Ronald J van der Sluis; Clara C Blad; Henk de Vries; Adriaan P IJzerman; Menno Hoekstra
Effects of pyrazole partial agonists on HCA(2) -mediated flushing and VLDL-triglyceride levels in mice.
British journal of pharmacology 2012;167(4):818-25.
2012: Ilze Bot; Martine Bot; Henk de Vries; Amanda C Foks; Suzanne J A Korporaal; Johan Kuiper; Mariëtte N D Ter Borg; Theo J C van Berkel; Peter J Van Santbrink; Jacobus van Veldhoven; Adriaan P IJzerman
Adenosine A₂B receptor agonism inhibits neointimal lesion development after arterial injury in apolipoprotein E-deficient mice.
Arteriosclerosis, thrombosis, and vascular biology 2012;32(9):2197-205.
2012: Gerard J P van Westen; Jörg K Wegner; Henk de Vries; Adriaan P IJzerman; Thea Mulder-Krieger; Olaf O van den Hoven; Rianne van der Pijl; Herman van Vlijmen; Andreas Bender
Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data.
Journal of medicinal chemistry 2012;55(16):7010-20.
2012: Wei Liu; Christopher B Roth; Aaron A Thompson; Fei Xu; Vadim Cherezov; Pavel Chubukov; Eugene Chun; Gye Won Han; Laura H Heitman; Adriaan P IJzerman; Vsevolod Katritch; Raymond C Stevens
Structural basis for allosteric regulation of GPCRs by sodium ions.
Science (New York, N.Y.) 2012;337(6091):232-6.
2012: M C Peeters; G Vriend; B Vroling; L E Wisse; A Dinaj; Adriaan P IJzerman
The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation.
Biochemical pharmacology 2012;84(1):76-87.
2012: Dong Guo; Adriaan P IJzerman; Thea Mulder-Krieger; Laura Heitman
Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time.
British journal of pharmacology 2012;166(6):1846-59.
2012: Marijn P A Sanders; Eelke van der Horst; Jody van Offenbeek; Stefan Verhoeven; Folkert Verkaar; Henry Vischer; Guido J R Zaman; Andreas Bender; Margot W Beukers; Ken Y Chow; Iwan J P De Esch; Jacob de Vlieg; Henk de Vries; Adriaan P IJzerman; Jan P G Klomp; J Robert Lane; Rob Leurs; Ross McGuire; Luc Roumen; Chris de Graaf
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design.
Journal of medicinal chemistry 2012;55(11):5311-25.
2012: Clara C Blad; Johannes Brussee; Corné Klopman; J Robert Lane; Jacobus P D van Veldhoven; Dieter R Wolfram; Adriaan P IJzerman
Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A).
Journal of medicinal chemistry 2012;55(7):3563-7.
2012: Laura Heitman; Gunnar Kleinau; Gerd Krause; Johannes Brussee; Adriaan P IJzerman
Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands.
Molecular and cellular endocrinology 2012;351(2):326-36.
2012: J Robert Lane; Jelle A Spoorendonk; Gerard van Westen; Carsten Hoffmann; Carmen Klein Herenbrink; Adriaan P IJzerman
A novel nonribose agonist, LUF5834, engages residues that are distinct from those of adenosine-like ligands to activate the adenosine A(2a) receptor.
Molecular pharmacology 2012;81(3):475-87.
2011: Eelke van der Horst; Rianne van der Pijl; Andreas Bender; Thea Mulder-Krieger; Adriaan P IJzerman
Substructure-based virtual screening for adenosine A2A receptor ligands.
ChemMedChem 2011;6(12):2302-11.
2011: Clara C Blad; Henk de Vries; Pnina Fishman; Thea Mulder-Krieger; Jacobien K Von Frijtag Drabbe Künzel; Sara Bar-Yehuda; Adriaan P IJzerman
Putative role of the adenosine A(3) receptor in the antiproliferative action of N (6)-(2-isopentenyl)adenosine.
Purinergic signalling 2011;7(4):453-62.
2011: Zhan-Guo Gao; Anikó Göblyös; Adriaan P IJzerman; Dennis Verzijl; Kai Ye; Annelien Zweemer; Kenneth Alan Jacobson
Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.
Biochemical pharmacology 2011;82(6):658-68.
2011: Stefan Offermanns; Steven L Colletti; Timothy W Lovenberg; Graeme Semple; Alan Wise; Adriaan P IJzerman
International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B).
Pharmacological reviews 2011;63(2):269-90.
2011: Ivone Gomes; Adriaan P IJzerman; Kai Ye; Emeline Maillet; Lakshmi A Devi
G protein-coupled receptor heteromerization: a role in allosteric modulation of ligand binding.
Molecular pharmacology 2011;79(6):1044-52.
2011: J P D van Veldhoven; C C Blad; C M Artsen; C Klopman; D R Wolfram; M J Abdelkadir; J R Lane; Johannes Brussee; Adriaan P IJzerman
Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).
Bioorganic & medicinal chemistry letters 2011;21(9):2736-9.
2011: Bertil B Fredholm; Adriaan P IJzerman; Kenneth Alan Jacobson; Joel Linden; Christa E Müller
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
Pharmacological reviews 2011;63(1):1-34.
2011: Miriam C Peeters; Gerard van Westen; Dong Guo; Lisanne E Wisse; Christa E Müller; Margot W Beukers; Adriaan P IJzerman
GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2011;25(2):632-43.
2011: Gerard van Westen; Inge Vereycken; Jörg K Wegner; Peggy Geluykens; Adriaan P IJzerman; Leen Kwanten; Anik Peeters; Herman van Vlijmen; Andreas Bender
Which compound to select in lead optimization? Prospectively validated proteochemometric models guide preclinical development.
PloS one 2011;6(11):e27518.
2011: Kenneth Alan Jacobson; Zhan-Guo Gao; Anikó Göblyös; Adriaan P IJzerman
Allosteric modulation of purine and pyrimidine receptors.
Advances in pharmacology (San Diego, Calif.) 2011;61():187-220.
2011: J Robert Lane; Veli-Pekka Jaakola; Adriaan P IJzerman
The structure of the adenosine receptors: implications for drug discovery.
Advances in pharmacology (San Diego, Calif.) 2011;61():1-40.
2011: M C Peeters; Gerard van Westen; Q Li; Adriaan P IJzerman
Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation.
Trends in pharmacological sciences 2011;32(1):35-42.
2010: J Robert Lane; Elisabeth Klaasse; Judy Lin; John van Bruchem; Margot W Beukers; Adriaan P IJzerman
Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor.
Biochemical pharmacology 2010;80(8):1180-9.
2010: Veli-Pekka Jaakola; Adriaan P IJzerman
The crystallographic structure of the human adenosine A2A receptor in a high-affinity antagonist-bound state: implications for GPCR drug screening and design.
Current opinion in structural biology 2010;20(4):401-14.
2010: Munikumar R Doddareddy; Elisabeth C Klaasse; Adriaan P IJzerman; Andreas Bender
Prospective validation of a comprehensive in silico hERG model and its applications to commercial compound and drug databases.
ChemMedChem 2010;5(5):716-29.
2010: Veli-Pekka Jaakola; J Robert Lane; Judy Y Lin; Vsevolod Katritch; Adriaan P IJzerman; Raymond C Stevens
Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues.
The Journal of biological chemistry 2010;285(17):13032-44.
2010: Rajeshwar Narlawar; J Robert Lane; Munikumar Doddareddy; Judy Lin; Johannes Brussee; Adriaan P IJzerman
Hybrid ortho/allosteric ligands for the adenosine A(1) receptor.
Journal of medicinal chemistry 2010;53(8):3028-37.
2010: Gerard van Westen; Joerg Wegner; Andreas Bender; Adriaan P IJzerman; Herman van Vlijmen
Mining protein dynamics from sets of crystal structures using "consensus structures".
Protein science : a publication of the Protein Society 2010;19(4):742-52.
2010: Vsevolod Katritch; Veli-Pekka Jaakola; J Robert Lane; Judy Lin; Adriaan P IJzerman; Mark Yeager; Irina Kufareva; Raymond C Stevens; Ruben Abagyan
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists.
Journal of medicinal chemistry 2010;53(4):1799-809.
2010: Eelke van der Horst; Julio Peironcely; Adriaan P IJzerman; Margot W Beukers; Jonathan R Lane; Herman van Vlijmen; Michael T M Emmerich; Yasushi Okuno; Andreas Bender
A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization.
BMC bioinformatics 2010;11():316.
2010: J Robert Lane; Margot W Beukers; Thea Mulder-Krieger; Adriaan P IJzerman
The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor.
Biochemical pharmacology 2010;79(1):48-56.
2009: Dong Guo; Elisabeth Klaasse; Henk de Vries; Johannes Brussee; Lukás Nalos; Martin B Rook; Marc A Vos; Marcel A G van der Heyden; Adriaan P IJzerman
Exploring chemical substructures essential for HERG k(+) channel blockade by synthesis and biological evaluation of dofetilide analogues.
ChemMedChem 2009;4(10):1722-32.
2009: Laura Heitman; Rajeshwar Narlawar; Henk de Vries; Milou N Willemsen; Dieter Wolfram; Johannes Brussee; Adriaan P IJzerman
Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.
Journal of medicinal chemistry 2009;52(7):2036-42.
2009: Yoonkyung Kim; Sonia De Castro; Zhan-Guo Gao; Adriaan P IJzerman; Kenneth Alan Jacobson
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
Journal of medicinal chemistry 2009;52(7):2098-108.
2009: Laura Heitman; Anikó Göblyös; Annelien M Zweemer; Renée Bakker; Thea Mulder-Krieger; Jacobus P D van Veldhoven; Henk de Vries; Johannes Brussee; Adriaan P IJzerman
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
Journal of medicinal chemistry 2009;52(4):926-31.
2009: Eelke van der Horst; Yasushi Okuno; Andreas Bender; Adriaan P IJzerman
Substructure mining of GPCR ligands reveals activity-class specific functional groups in an unbiased manner.
Journal of chemical information and modeling 2009;49(2):348-60.
2009: Nancy Dewi Yuliana; Alfi Khatib; Anne Maria Link-Struensee; Adriaan P IJzerman; Fransiska Rungkat-Zakaria; Young Hae Choi; Robert Verpoorte
Adenosine A1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus.
Planta medica 2009;75(2):132-6.
2008: Veli-Pekka Jaakola; Mark T Griffith; Michael A Hanson; Vadim Cherezov; Ellen Y T Chien; J Robert Lane; Adriaan P IJzerman; Raymond C Stevens
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.
Science (New York, N.Y.) 2008;322(5905):1211-7.
2008: Laura Heitman; Adriaan P IJzerman
G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: a case for Gnrh, LH, FSH, and GPR54 receptor ligands.
Medicinal research reviews 2008;28(6):975-1011.
2008: Laura Heitman; Jacobus P D van Veldhoven; Annelien M Zweemer; Kai Ye; Johannes Brussee; Adriaan P IJzerman
False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase.
Journal of medicinal chemistry 2008;51(15):4724-9.
2008: Monica Mantri; Olivier de Graaf; Jacobus van Veldhoven; Anikó Göblyös; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Regina Link; Henk de Vries; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Journal of medicinal chemistry 2008;51(15):4449-55.
2008: Laura Heitman; Kai Ye; Julia Oosterom; Adriaan P IJzerman
Amiloride derivatives and a nonpeptidic antagonist bind at two distinct allosteric sites in the human gonadotropin-releasing hormone receptor.
Molecular pharmacology 2008;73(6):1808-15.
2008: Kai Ye; Gert Vriend; Adriaan P IJzerman
Tracing evolutionary pressure.
Bioinformatics (Oxford, England) 2008;24(7):908-15.
2008: Kimberly M Bonger; Richard J B H N van den Berg; Annemiek D Knijnenburg; Laura Heitman; Adriaan P IJzerman; Julia Oosterom; Cornelis M Timmers; Herman S Overkleeft; Gijsbert A van der Marel
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.
Bioorganic & medicinal chemistry 2008;16(7):3744-58.
2008: Jacobus P D van Veldhoven; Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Regina Struensee-Link; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Bioorganic & medicinal chemistry 2008;16(6):2741-52.
2008: Elisabeth C Klaasse; Adriaan P IJzerman; Willem J De Grip; Margot W Beukers
Internalization and desensitization of adenosine receptors.
Purinergic signalling 2008;4(1):21-37.
2008: Laura Heitman; Julia Oosterom; Kimberly M Bonger; Cornelis M Timmers; Peter H G Wiegerinck; Adriaan P IJzerman
[3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor.
Molecular pharmacology 2008;73(2):518-24.
2008: Zhan-Guo Gao; Kai Ye; Anikó Göblyös; Adriaan P IJzerman; Kenneth Alan Jacobson
Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000.
BMC pharmacology 2008;8():20.
2008: Kai Ye; K Anton Feenstra; Jaap Heringa; Adriaan P IJzerman; Elena Marchiori
Multi-RELIEF: a method to recognize specificity determining residues from multiple sequence alignments using a Machine-Learning approach for feature weighting.
Bioinformatics (Oxford, England) 2008;24(1):18-25.
2008: Eva-María Priego; María-Jesús Pérez-Pérez; Jacobien K von Frijtag Drabbe Kuenzel; Henk de Vries; Adriaan P IJzerman; María-José Camarasa; Sonsoles Martín-Santamaría
Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding.
ChemMedChem 2008;3(1):111-9.
2008: Jeroen Kazius; Kerstin Wurdinger; Maarten van Iterson; Joost Kok; Thomas Bäck; Adriaan P IJzerman
GPCR NaVa database: natural variants in human G protein-coupled receptors.
Human mutation 2008;29(1):39-44.
2007: Kimberly M Bonger; Richard J B H N van den Berg; Laura Heitman; Adriaan P IJzerman; Julia Oosterom; Cornelis M Timmers; Herman S Overkleeft; Gijsbert A van der Marel
Synthesis and evaluation of homo-bivalent GnRHR ligands.
Bioorganic & medicinal chemistry 2007;15(14):4841-56.
2007: Willem Soudijn; Ineke van Wijngaarden; Adriaan P IJzerman
Nicotinic acid receptor subtypes and their ligands.
Medicinal research reviews 2007;27(3):417-33.
2007: Eric-Wubbo Lameijer; Reynier A Tromp; Ronald F Spanjersberg; Johannes Brussee; Adriaan P IJzerman
Designing active template molecules by combining computational de novo design and human chemist's expertise.
Journal of medicinal chemistry 2007;50(8):1925-32.
2007: Elena V Samsonova; Peter Krause; Thomas Bäck; Adriaan P IJzerman
Characteristic amino acid combinations in olfactory G protein-coupled receptors.
Proteins 2007;67(1):154-66.
2007: Kai Ye; Walter A Kosters; Adriaan P IJzerman
An efficient, versatile and scalable pattern growth approach to mine frequent patterns in unaligned protein sequences.
Bioinformatics (Oxford, England) 2007;23(6):687-93.
2007: Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Joost Westerhout; Thomas Spangenberg; Johannes Brussee; Adriaan P IJzerman
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Journal of medicinal chemistry 2007;50(4):828-34.
2007: Qilan Li; Kai Ye; Clara C Blad; Hans den Dulk; Jaap Brouwer; Adriaan P IJzerman; Margot W Beukers
ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.
The Journal of pharmacology and experimental therapeutics 2007;320(2):637-45.
2006: Margot W Beukers; Illiana Meurs; Adriaan P IJzerman
Structure-affinity relationships of adenosine A2B receptor ligands.
Medicinal research reviews 2006;26(5):667-98.
2006: Elena V Samsonova; Joost N Kok; Adriaan P IJzerman
TreeSOM: Cluster analysis in the self-organizing map.
Neural networks : the official journal of the International Neural Network Society 2006;19(6-7):935-49.
2006: Anikó Göblyös; Zhan-Guo Gao; Johannes Brussee; Roberto Connestari; Sabrina Neves Santiago; Kai Ye; Adriaan P IJzerman; Kenneth Alan Jacobson
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Journal of medicinal chemistry 2006;49(11):3354-61.
2006: Kai Ye; Eric-Wubbo M Lameijer; Margot W Beukers; Adriaan P IJzerman
A two-entropies analysis to identify functional positions in the transmembrane region of class A G protein-coupled receptors.
Proteins 2006;63(4):1018-30.
2006: Lisa C W Chang; Ronald F Spanjersberg; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Johannes Brussee; Adriaan P IJzerman
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Journal of medicinal chemistry 2006;49(10):2861-7.
2006: Jeroen Kazius; Siegfried Nijssen; Joost Kok; Thomas Bäck; Adriaan P IJzerman
Substructure mining using elaborate chemical representation.
Journal of chemical information and modeling 2006;46(2):597-605.
2006: Eric-Wubbo Lameijer; Joost N Kok; Thomas Bäck; Adriaan P IJzerman
Mining a chemical database for fragment co-occurrence: discovery of "chemical clichés".
Journal of chemical information and modeling 2006;46(2):553-62.
2006: Eric-Wubbo Lameijer; Joost N Kok; Thomas Bäck; Adriaan P IJzerman
The molecule evoluator. An interactive evolutionary algorithm for the design of drug-like molecules.
Journal of chemical information and modeling 2006;46(2):545-52.
2006: Laura Heitman; Thea Mulder-Krieger; Ronald F Spanjersberg; Jacobien K Von Frijtag Drabbe Künzel; Alessandro Dalpiaz; Adriaan P IJzerman
Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.
British journal of pharmacology 2006;147(5):533-41.
2006: Richard A Bond; Adriaan P IJzerman
Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery.
Trends in pharmacological sciences 2006;27(2):92-6.
2005: Elisabeth C Klaasse; Gijs van den Hout; Sophie F Roerink; Willem J De Grip; Adriaan P IJzerman; Margot W Beukers
Allosteric modulators affect the internalization of human adenosine A1 receptors.
European journal of pharmacology 2005;522(1-3):1-8.
2005: Margot W Beukers; Adriaan P IJzerman
Techniques: how to boost GPCR mutagenesis studies using yeast.
Trends in pharmacological sciences 2005;26(10):533-9.
2005: Willem Soudijn; Ineke van Wijngaarden; Adriaan P IJzerman
Structure-activity relationships of inverse agonists for G-protein-coupled receptors.
Medicinal research reviews 2005;25(4):398-426.
2005: Zhan-Guo Gao; Soo-Kyung Kim; Adriaan P IJzerman; Kenneth Alan Jacobson
Allosteric modulation of the adenosine family of receptors.
Mini reviews in medicinal chemistry 2005;5(6):545-53.
2005: Marloes P Schaddelee; Sue D Collins; Joost DeJongh; Albertus G de Boer; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic/pharmacodynamic modelling of the anti-hyperalgesic and anti-nociceptive effect of adenosine A1 receptor partial agonists in neuropathic pain.
European journal of pharmacology 2005;514(2-3):131-40.
2005: Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Ronald F Spanjersberg; Sophie F Roerink; Gijs van den Hout; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Journal of medicinal chemistry 2005;48(6):2045-53.
2005: Anikó Göblyös; Sabrina Neves Santiago; Daniele Pietra; Thea Mulder-Krieger; Jacobien K Von Frijtag Drabbe Künzel; Johannes Brussee; Adriaan P IJzerman
Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers.
Bioorganic & medicinal chemistry 2005;13(6):2079-87.
2005: Rianne A F de Ligt; Scott A Rivkees; Anna Lorenzen; Rob Leurs; Adriaan P IJzerman
A "locked-on," constitutively active mutant of the adenosine A1 receptor.
European journal of pharmacology 2005;510(1-2):1-8.
2005: Anikó Göblyös; Henk de Vries; Johannes Brussee; Adriaan P IJzerman
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
Journal of medicinal chemistry 2005;48(4):1145-51.
2005: Reynier A Tromp; Ronald F Spanjersberg; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.
Journal of medicinal chemistry 2005;48(1):321-9.
2005: Marloes P Schaddelee; Kevin D Read; Cindy G J Cleypool; Adriaan P IJzerman; Meindert Danhof; Albertus G de Boer
Brain penetration of synthetic adenosine A1 receptor agonists in situ: role of the rENT1 nucleoside transporter and binding to blood constituents.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 2005;24(1):59-66.
2004: Lisa C W Chang; Ronald F Spanjersberg; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Gijs van den Hout; Margot W Beukers; Johannes Brussee; Adriaan P IJzerman
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Journal of medicinal chemistry 2004;47(26):6529-40.
2004: Marloes P Schaddelee; Dorien Groenendaal; Joost DeJongh; C G J Cleypool; Adriaan P IJzerman; Albertus G de Boer; Meindert Danhof
Population pharmacokinetic modeling of blood-brain barrier transport of synthetic adenosine A1 receptor agonists.
The Journal of pharmacology and experimental therapeutics 2004;311(3):1138-46.
2004: Marloes P Schaddelee; Joost DeJongh; Sue D Collins; Albertus G de Boer; Adriaan P IJzerman; Meindert Danhof
Population pharmacokinetic-pharmacodynamic modelling of the anti-hyperalgesic effect of 5'deoxy-N6-cylopentyladenosine in the mononeuropathic rat.
European journal of pharmacology 2004;504(1-2):7-15.
2004: Lisa C W Chang; Johannes Brussee; Adriaan P IJzerman
Non-xanthine antagonists for the adenosine A1 receptor.
Chemistry & biodiversity 2004;1(11):1591-626.
2004: Yolande Cordeaux; Adriaan P IJzerman; Stephen J Hill
Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist-specific G protein activation.
British journal of pharmacology 2004;143(6):705-14.
2004: Reynier A Tromp; Susan van Ameijde; Claudia Pütz; Corinna Sundermann; Bernd Sundermann; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups.
Journal of medicinal chemistry 2004;47(22):5441-50.
2004: Elisabeth C Klaasse; Rianne A F de Ligt; Sophie F Roerink; Anna Lorenzen; Graeme Milligan; Rob Leurs; Adriaan P IJzerman
Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits.
European journal of pharmacology 2004;499(1-2):91-8.
2004: Willem Soudijn; Ineke van Wijngaarden; Adriaan P IJzerman
Allosteric modulation of G protein-coupled receptors: perspectives and recent developments.
Drug discovery today 2004;9(17):752-8.
2004: Margot W Beukers; Lisa C W Chang; Jacobien K Von Frijtag Drabbe Künzel; Thea Mulder-Krieger; Ronald F Spanjersberg; Johannes Brussee; Adriaan P IJzerman
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
Journal of medicinal chemistry 2004;47(15):3707-9.
2004: Maria C Wittendorp; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman; Hendrikus W G M Boddeke; Knut Biber
The mouse brain adenosine A1 receptor: functional expression and pharmacology.
European journal of pharmacology 2004;487(1-3):73-9.
2004: Margot W Beukers; Joris van Oppenraaij; Patrick P W van der Hoorn; Clara C Blad; Hans den Dulk; Jaap Brouwer; Adriaan P IJzerman
Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations.
Molecular pharmacology 2004;65(3):702-10.
2004: Adrianus M C H van den Nieuwendijk; Daniele Pietra; Laura Heitman; Anikó Göblyös; Adriaan P IJzerman
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.
Journal of medicinal chemistry 2004;47(3):663-72.
2004: Rianne A F de Ligt; Pieter A M van der Klein; Jacobien K Von Frijtag Drabbe Künzel; Anna Lorenzen; Fatna Ait El Maate; Shelly Fujikawa; Rosemarijn van Westhoven; Thijs van den Hoven; Johannes Brussee; Adriaan P IJzerman
Synthesis and biological evaluation of disubstituted N6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 receptor.
Bioorganic & medicinal chemistry 2004;12(1):139-49.
2003: Tjerk J H Bueters; Leonie van Duivenvoorde; Meindert Danhof; Adriaan P IJzerman; Herman P M Van Helden
Cyclopentyladenosine and some of its low-efficacy derivatives inhibit striatal synaptosomal release of acetylcholine to a similar degree.
European journal of pharmacology 2003;481(2-3):141-6.
2003: Marloes P Schaddelee; Heleen L Voorwinden; Dorien Groenendaal; Anne Hersey; Adriaan P IJzerman; Meindert Danhof; Albertus G de Boer
Blood-brain barrier transport of synthetic adenosine A1 receptor agonists in vitro: structure transport relationships.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 2003;20(3):347-56.
2003: Tjerk J H Bueters; Adriaan P IJzerman; Herman P M Van Helden; Meindert Danhof
Characterization of the pharmacokinetics, brain distribution, and therapeutic efficacy of the adenosine A1 receptor partial agonist 2'-deoxy-N6-cyclopentyladenosine in sarin-poisoned rats.
Toxicology and applied pharmacology 2003;192(1):86-94.
2003: T van Herk; Johannes Brussee; Adrianus M C H van den Nieuwendijk; Pieter A M van der Klein; Adriaan P IJzerman; Christina Stannek; A Burmeister; Anna Lorenzen
Pyrazole derivatives as partial agonists for the nicotinic acid receptor.
Journal of medicinal chemistry 2003;46(18):3945-51.
2003: Patrick K Harrison; Tjerk J H Bueters; Adriaan P IJzerman; Herman P M Van Helden; John E H Tattersall
Partial adenosine A(1) receptor agonists inhibit sarin-induced epileptiform activity in the hippocampal slice.
European journal of pharmacology 2003;471(2):97-104.
2003: Tjerk J H Bueters; Herman P M Van Helden; Adriaan P IJzerman; Meindert Danhof
Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action.
Neuroscience letters 2003;343(1):57-61.
2003: Erica W van Tilburg; Matty Gremmen; Jacobien K Von Frijtag Drabbe Künzel; Miriam de Groote; Adriaan P IJzerman
2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor.
Bioorganic & medicinal chemistry 2003;11(10):2183-92.
2003: Marloes P Schaddelee; Heleen L Voorwinden; Erica W van Tilburg; Tony J Pateman; Adriaan P IJzerman; Meindert Danhof; Albertus G de Boer
Functional role of adenosine receptor subtypes in the regulation of blood-brain barrier permeability: possible implications for the design of synthetic adenosine derivatives.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 2003;19(1):13-22.
2003: Margot W Beukers; Martin J Wanner; Jacobien K Von Frijtag Drabbe Künzel; Elisabeth C Klaasse; Adriaan P IJzerman; Gerrit-Jan Koomen
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Journal of medicinal chemistry 2003;46(8):1492-503.
2003: Paymaneh Y F Deghati; Alice Borghini; Adrianus M C H van den Nieuwendijk; Miriam Dissen-de Groote; Adriaan P IJzerman
Inhibition of nucleoside transport by new analogues of nitrobenzylthioinosine.
Bioorganic & medicinal chemistry 2003;11(6):899-908.
2003: Tjerk J H Bueters; Marloes J A Joosen; Herman P M Van Helden; Adriaan P IJzerman; Meindert Danhof
Adenosine A1 receptor agonist N6-cyclopentyladenosine affects the inactivation of acetylcholinesterase in blood and brain by sarin.
The Journal of pharmacology and experimental therapeutics 2003;304(3):1307-13.
2003: Zhan-Guo Gao; Neli Melman; Andreas A Erdmann; Seong-Gon Kim; Christa E Müller; Adriaan P IJzerman; Kenneth Alan Jacobson
Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors.
Biochemical pharmacology 2003;65(4):525-34.
2003: Willem Soudjin; Ineke van Wijngaarden; Adriaan P IJzerman
Stereoselectivity of drug-receptor interactions.
IDrugs : the investigational drugs journal 2003;6(1):43-56.
2003: Willem Soudijn; Ineke van Wijngaarden; Adriaan P IJzerman
Medicinal chemistry of adenosine A1 receptor ligands.
Current topics in medicinal chemistry 2003;3(4):355-67.
2002: Tjerk J H Bueters; Herman P M Van Helden; Meindert Danhof; Adriaan P IJzerman
Effects of the adenosine A1 receptor allosteric modulators PD 81,723 and LUF 5484 on the striatal acetylcholine release.
European journal of pharmacology 2002;454(2-3):177-82.
2002: Tjerk J H Bueters; Bas Groen; Meindert Danhof; Adriaan P IJzerman; Herman P M Van Helden
Therapeutic efficacy of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) against organophosphate intoxication.
Archives of toxicology 2002;76(11):650-6.
2002: Anna Lorenzen; Margot W Beukers; Piet Hein van der Graaf; Heidrun Lang; Jacqueline van Muijlwijk-Koezen; Miriam de Groote; Wiro M P B Menge; Ulrich Schwabe; Adriaan P IJzerman
Modulation of agonist responses at the A(1) adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state.
Biochemical pharmacology 2002;64(8):1251-65.
2002: Willem Soudijn; Ineke van Wijngaarden; Adriaan P IJzerman
Allosteric modulation of G protein-coupled receptors.
Current opinion in drug discovery & development 2002;5(5):749-55.
2002: Eva-María Priego; Jacobien von Frijtag Drabbe Kuenzel; Adriaan P IJzerman; María-José Camarasa; María-Jesús Pérez-Pérez
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Journal of medicinal chemistry 2002;45(16):3337-44.
2002: Alessandro Dalpiaz; Barbara Pavan; Françoise Ngo Ngos; Palmarisa Franchetti; Adriaan P IJzerman
Temperature dependence of the affinity enhancement of selective adenosine A1 receptor agonism: a thermodynamic analysis.
European journal of pharmacology 2002;448(2-3):123-31.
2002: Zhan-Guo Gao; Seong-Gon Kim; Kelly A Soltysiak; Neli Melman; Adriaan P IJzerman; Kenneth Alan Jacobson
Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives.
Molecular pharmacology 2002;62(1):81-9.
2002: Serge Van Calenbergh; Andreas Link; Shelly Fujikawa; Rianne A F de Ligt; Veerle Vanheusden; Abolfasl Golisade; Norbert Blaton; Jef Rozenski; Adriaan P IJzerman; Piet Herdewijn
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
Journal of medicinal chemistry 2002;45(9):1845-52.
2002: Renata Del Carmine; Caterina Ambrosio; Maria Sbraccia; Susanna Cotecchia; Adriaan P IJzerman; Tommaso Costa
Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the beta(2)-adrenergic receptor.
British journal of pharmacology 2002;135(7):1715-22.
2002: S Mariëtte Schrier; Bogdan I Florea; Gerard J Mulder; J Fred Nagelkerke; Adriaan P IJzerman
Apoptosis induced by extracellular ATP in the mouse neuroblastoma cell line N1E-115: studies on involvement of P2 receptors and adenosine.
Biochemical pharmacology 2002;63(6):1119-26.
2002: Joke M M den Haan; Tuna Mutis; Els Blokland; Adriaan P IJzerman; Els Goulmy
General T-cell receptor antagonists to immunomodulate HLA-A2-restricted minor histocompatibility antigen HA-1-specific T-cell responses.
Blood 2002;99(3):985-92.
2002: Erica W van Tilburg; Jacobien von Frijtag Drabbe Kunzel; Miriam de Groote; Adriaan P IJzerman
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Journal of medicinal chemistry 2002;45(2):420-9.
2002: Rianne A F de Ligt; Adriaan P IJzerman
Intrinsic activity at adenosine A1 receptors: partial and inverse agonism.
Current pharmaceutical design 2002;8(26):2333-44.
2001: Bertil B. Fredholm; Adriaan P IJzerman; Kenneth Alan Jacobson; Karl-Norbert Klotz; J Linden
International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors.
Pharmacological reviews 2001;53(4):527-52.
2001: Zhan-Guo Gao; J E Van Muijlwijk-Koezen; Aishe Chen; Christa E Müller; Adriaan P IJzerman; Kenneth Alan Jacobson
Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives.
Molecular pharmacology 2001;60(5):1057-63.
2001: Erica W van Tilburg; Pieter A M van der Klein; Jacobien K Von Frijtag Drabbe Künzel; Miriam de Groote; Christina Stannek; Anna Lorenzen; Adriaan P IJzerman
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
Journal of medicinal chemistry 2001;44(18):2966-75.
2001: Erica W van Tilburg; Pieter A M van der Klein; Miriam de Groote; Margot W Beukers; Adriaan P IJzerman
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Bioorganic & medicinal chemistry letters 2001;11(15):2017-9.
2001: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; R P van der Sluis; Andrea C van de Stolpe; Wiro M P B Menge; Margot W Beukers; Piet Hein van der Graaf; Miriam de Groote; Adriaan P IJzerman
Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool.
Bioorganic & medicinal chemistry letters 2001;11(6):815-8.
2001: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; Roeland C Vollinga; J Frijtag von Drabbe Künzel; Miriam de Groote; Sandra A G Visser; Adriaan P IJzerman
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
Journal of medicinal chemistry 2001;44(5):749-62.
2001: S Mariëtte Schrier; E W van Tilburg; Hans van der Meulen; Adriaan P IJzerman; Gerard J Mulder; J Fred Nagelkerke
Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells: studies on involvement of adenosine receptors and adenosine uptake.
Biochemical pharmacology 2001;61(4):417-25.
2001: AP Kourounakis; C Visser; Miriam de Groote; Adriaan P IJzerman
Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor.
Biochemical pharmacology 2001;61(2):137-44.
2001: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; Adriaan P IJzerman
The adenosine A3 receptor and its ligands.
Progress in medicinal chemistry 2001;38():61-113.
2001: Adriaan P IJzerman; AP Kourounakis; Pieter A M van der Klein
Allosteric modulation of G protein-coupled receptors.
Farmaco (Società chimica italiana : 1989) 2001;56(1-2):67-70.
2000: Margot W Beukers; Hans den Dulk; Erica W van Tilburg; Jaap Brouwer; Adriaan P IJzerman
Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Molecular pharmacology 2000;58(6):1349-56.
2000: Martin J Wanner; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman; Gerrit-Jan Koomen
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.
Bioorganic & medicinal chemistry letters 2000;10(18):2141-4.
2000: Zhan-Guo Gao; Adriaan P IJzerman
Allosteric modulation of A(2A) adenosine receptors by amiloride analogues and sodium ions.
Biochemical pharmacology 2000;60(5):669-76.
2000: Zhan-Guo Gao; Q Jiang; Kenneth Alan Jacobson; Adriaan P IJzerman
Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation.
Biochemical pharmacology 2000;60(5):661-8.
2000: M Garrido; Josy M Gubbens-Stibbe; EJ Tukker; E Cox; J von Frijtag; D Künzel; Adriaan P IJzerman; Meindert Danhof; Piet H van Der Graaf
Pharmacokinetic-pharmacodynamic analysis of the EEG effect of alfentanil in rats following beta-funaltrexamine-induced mu-opioid receptor "knockdown" in vivo.
Pharmaceutical research 2000;17(6):653-9.
2000: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; Henk van der Goot; Wiro M P B Menge; J Frijtag Von Drabbe Künzel; Miriam de Groote; Adriaan P IJzerman
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Journal of medicinal chemistry 2000;43(11):2227-38.
2000: R A de Ligt; A P Kourounakis; Adriaan P IJzerman
Inverse agonism at G protein-coupled receptors: (patho)physiological relevance and implications for drug discovery.
British journal of pharmacology 2000;130(1):1-12.
2000: Kornkanok Ingkaninan; Adriaan P IJzerman; Robert Verpoorte
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.
Journal of natural products 2000;63(3):315-7.
2000: Sauro Vittori; Anna Lorenzen; Christina Stannek; Stefano Costanzi; Rosaria Volpini; Adriaan P IJzerman; J K Kunzel; Gloria Cristalli
N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor.
Journal of medicinal chemistry 2000;43(2):250-60.
2000: S M Schier; Adriaan P IJzerman; Gerard J Mulder; J Fred Nagelkerke
Adenosine-induced caspase activity in N1E-115 cells.
Advances in experimental medicine and biology 2000;486():223-6.
1999: Kornkanok Ingkaninan; Adriaan P IJzerman; T Taesotikult; Robert Verpoorte
Isolation of opioid-active compounds from Tabernaemontana pachysiphon leaves.
The Journal of pharmacy and pharmacology 1999;51(12):1441-6.
1999: Margot W Beukers; I Kristiansen; Adriaan P IJzerman; I Edvardsen
TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data.
Trends in pharmacological sciences 1999;20(12):475-7.
1999: H M Zuurmond; J Hessling; K Blüml; M Lohse; Adriaan P IJzerman
Study of interaction between agonists and asn293 in helix VI of human beta(2)-adrenergic receptor.
Molecular pharmacology 1999;56(5):909-16.
1999: Pieter A M van der Klein; AP Kourounakis; Adriaan P IJzerman
Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.
Journal of medicinal chemistry 1999;42(18):3629-35.
1999: Piet H van Der Graaf; EA van Schaick; Sandra A G Visser; HJ de Greef; Adriaan P IJzerman; Meindert Danhof
Mechanism-based pharmacokinetic-pharmacodynamic modeling of antilipolytic effects of adenosine A(1) receptor agonists in rats: prediction of tissue-dependent efficacy in vivo.
The Journal of pharmacology and experimental therapeutics 1999;290(2):702-9.
1999: Kornkanok Ingkaninan; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman; Robert Verpoorte
Interference of linoleic acid fraction in some receptor binding assays.
Journal of natural products 1999;62(6):912-4.
1999: Erica W van Tilburg; Jacobien K Von Frijtag Drabbe Künzel; Miriam de Groote; Roeland C Vollinga; Anna Lorenzen; Adriaan P IJzerman
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
Journal of medicinal chemistry 1999;42(8):1393-400.
1999: M de Zwart; AP Kourounakis; Huub Kooijman; Anthony L Spek; R Link; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Journal of medicinal chemistry 1999;42(8):1384-92.
1998: B Pavan; Adriaan P IJzerman
Processing of adenosine receptor agonists in rat and human whole blood.
Biochemical pharmacology 1998;56(12):1625-32.
1998: A Dalpiaz; A Townsend-Nicholson; Margot W Beukers; PR Schofield; Adriaan P IJzerman
Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors.
Biochemical pharmacology 1998;56(11):1437-45.
1998: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; R Link; Henk van der Goot; Adriaan P IJzerman
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Journal of medicinal chemistry 1998;41(21):3994-4000.
1998: Jacqueline van Muijlwijk-Koezen; Henk Timmerman; R Link; Henk van der Goot; Adriaan P IJzerman
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Journal of medicinal chemistry 1998;41(21):3987-93.
1998: EA van Schaick; Klaas P Zuideveld; H E Tukker; MW Langemeijer; Adriaan P IJzerman; Meindert Danhof
Metabolic and cardiovascular effects of the adenosine A1 receptor agonist N6-(p-sulfophenyl)adenosine in diabetic Zucker rats: influence of the disease on the selectivity of action.
The Journal of pharmacology and experimental therapeutics 1998;287(1):21-30.
1998: YC Kim; M de Zwart; LengChee Chang; Stefano Moro; Jacobien K Von Frijtag Drabbe Künzel; Neli Melman; Adriaan P IJzerman; Kenneth Alan Jacobson
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
Journal of medicinal chemistry 1998;41(15):2835-45.
1998: M de Zwart; R Link; Jacobien K Von Frijtag Drabbe Künzel; G Cristalli; Kenneth Alan Jacobson; A Townsend-Nicholson; Adriaan P IJzerman
A functional screening of adenosine analogues at the adenosine A2B receptor: a search for potent agonists.
Nucleosides & nucleotides 1998;17(6):969-85.
1998: EA van Schaick; H E Tukker; H C Roelen; Adriaan P IJzerman; Meindert Danhof
Selectivity of action of 8-alkylamino analogues of N6-cyclopentyladenosine in vivo: haemodynamic versus anti-lipolytic responses in rats.
British journal of pharmacology 1998;124(3):607-18.
1998: Joke A Bouwstra; Gert S Gooris; Frank E R Dubbelaar; Arij M Weerheim; Adriaan P IJzerman; Maria Ponec
Role of ceramide 1 in the molecular organization of the stratum corneum lipids.
Journal of lipid research 1998;39(1):186-96.
1998: E M van der Wenden; M Carnielli; H C Roelen; Anna Lorenzen; Jacobien K Von Frijtag Drabbe Künzel; Adriaan P IJzerman
5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor.
Journal of medicinal chemistry 1998;41(1):102-8.
1997: EA van Schaick; HJ de Greef; Adriaan P IJzerman; Meindert Danhof
Physiological indirect effect modeling of the antilipolytic effects of adenosine A1-receptor agonists.
Journal of pharmacokinetics and biopharmaceutics 1997;25(6):673-94.
1997: EA van Schaick; C Kulkarni; Jacobien K Von Frijtag Drabbe Künzel; R A Mathôt; G Cristalli; Adriaan P IJzerman; Meindert Danhof
Time course of action of three adenosine A1 receptor agonists with differing lipophilicity in rats: comparison of pharmacokinetic, haemodynamic and EEG effects.
Naunyn-Schmiedeberg's archives of pharmacology 1997;356(6):827-37.
1997: Serge Van Calenbergh; J K von Frijtag Drabbe Künzel; Norbert Blaton; Oswald M Peeters; Jef Rozenski; A Van Aerschot; A De Bruyn; Denis De Keukeleire; Adriaan P IJzerman; Piet Herdewijn
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.
Journal of medicinal chemistry 1997;40(23):3765-72.
1997: Piet H van Der Graaf; EA van Schaick; R A Math-ot; Adriaan P IJzerman; Meindert Danhof
Mechanism-based pharmacokinetic-pharmacodynamic modeling of the effects of N6-cyclopentyladenosine analogs on heart rate in rat: estimation of in vivo operational affinity and efficacy at adenosine A1 receptors.
The Journal of pharmacology and experimental therapeutics 1997;283(2):809-16.
1997: EA van Schaick; R A Math-ot; Josy M Gubbens-Stibbe; MW Langemeijer; H C Roelen; Adriaan P IJzerman; Meindert Danhof
8-Alkylamino-substituted analogs of N6-cyclopentyladenosine are partial agonists for the cardiovascular adenosine A1 receptors in vivo.
The Journal of pharmacology and experimental therapeutics 1997;283(2):800-8.
1997: EA van Schaick; HJ de Greef; MW Langemeijer; M J Sheehan; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic and anti-ketotic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine in rats.
British journal of pharmacology 1997;122(3):525-33.
1997: Anna Lorenzen; Ana M Sebastião; A Sellink; H Vogt; Ulrich Schwabe; Joaquim Alexandre Ribeiro; Adriaan P IJzerman
Biological activities of N6,C8-disubstituted adenosine derivatives as partial agonists at rat brain adenosine A1 receptors.
European journal of pharmacology 1997;334(2-3):299-307.
1997: W Kuipers; L Oliveira; G Vriend; Adriaan P IJzerman
Identification of class-determining residues in G protein-coupled receptors by sequence analysis.
Receptors & channels 1997;5(3-4):159-74.
1996: R A Mathot; E M Wenden; Willem Soudijn; Douwe D Breimer; Adriaan P IJzerman; Meindert Danhof
Partial agonism of the nonselective adenosine receptor agonist 8-butylaminoadenosine at the A1 receptor in vivo.
The Journal of pharmacology and experimental therapeutics 1996;279(3):1439-46.
1996: Adriaan P IJzerman; Jacobien K Von Frijtag Drabbe Künzel; J Kim; Q Jiang; Kenneth Alan Jacobson
Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition.
European journal of pharmacology 1996;310(2-3):269-72.
1996: EA van Schaick; Kenneth Alan Jacobson; H O Kim; Adriaan P IJzerman; Meindert Danhof
Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats.
European journal of pharmacology 1996;308(3):311-4.
1996: R A Mathoôt; Willem Soudijn; Douwe D Breimer; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic-haemodynamic relationships of 2-chloroadenosine at adenosine A1 and A2a receptors in vivo.
British journal of pharmacology 1996;118(2):369-77.
1996: H Roelen; N Veldman; A L Spek; Jacobien K Von Frijtag Drabbe Künzel; R A Mathôt; Adriaan P IJzerman
N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors.
Journal of medicinal chemistry 1996;39(7):1463-71.
1995: R A Mathôt; E M Van der Wenden; Willem Soudijn; Adriaan P IJzerman; Meindert Danhof
Deoxyribose analogues of N6-cyclopentyladenosine (CPA): partial agonists at the adenosine A1 receptor in vivo.
British journal of pharmacology 1995;116(3):1957-64.
1995: R A Mathôt; Josy M Gubbens-Stibbe; Willem Soudijn; Kenneth Alan Jacobson; Adriaan P IJzerman; Meindert Danhof
Quantification of the in vivo potency of the adenosine A2 receptor antagonist 8-(3-chlorostyryl)caffeine.
The Journal of pharmacology and experimental therapeutics 1995;275(1):245-53.
1995: E M van der Wenden; Jacobien K Von Frijtag Drabbe Künzel; R A Mathôt; Meindert Danhof; Adriaan P IJzerman; Willem Soudijn
Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor.
Journal of medicinal chemistry 1995;38(20):4000-6.
1995: E M Van der Wenden; H R Hartog-Witte; H C Roelen; Jacobien K Von Frijtag Drabbe Künzel; I M Pirovano; R A Mathôt; Meindert Danhof; Arthur Van Aerschot; M J Lidaks; Adriaan P IJzerman
8-substituted adenosine and theophylline-7-riboside analogues as potential partial agonists for the adenosine A1 receptor.
European journal of pharmacology 1995;290(3):189-99.
1995: S Appel; R A Mathôt; MW Langemeijer; Adriaan P IJzerman; Meindert Danhof
Modelling of the pharmacodynamic interaction of an A1 adenosine receptor agonist and antagonist in vivo: N6-cyclopentyladenosine and 8-cyclopentyltheophylline.
British journal of pharmacology 1995;115(7):1253-9.
1995: W Kuipers; Ineke van Wijngaarden; Chris G Kruse; M ter Horst-van Amstel; Martin Tulp; Adriaan P IJzerman
N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands.
Journal of medicinal chemistry 1995;38(11):1942-54.
1995: Margot W Beukers; C J Kerkhof; M A van Rhee; U Ardanuy; C Gurgel; H Widjaja; Peter Nickel; Adriaan P IJzerman; Willem Soudijn
Suramin analogs, divalent cations and ATP gamma S as inhibitors of ecto-ATPase.
Naunyn-Schmiedeberg's archives of pharmacology 1995;351(5):523-8.
1995: R A Mathôt; B C Van den Aarsen; Willem Soudijn; Douwe D Breimer; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic-pharmacodynamic modelling of the cardiovascular effects of R- and S-N6-phenylisopropyladenosine in conscious normotensive rats.
The Journal of pharmacology and experimental therapeutics 1995;273(1):405-14.
1995: R A Mathôt; Anne-Marie Cleton; Willem Soudijn; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic modelling of the haemodynamic effects of the A2a adenosine receptor agonist CGS 21680C in conscious normotensive rats.
British journal of pharmacology 1995;114(4):761-8.
1995: E M van der Wenden; Sarah L Price; R P Apaya; Adriaan P IJzerman; Willem Soudijn
Relative binding orientations of adenosine A1 receptor ligands--a test case for Distributed Multipole Analysis in medicinal chemistry.
Journal of computer-aided molecular design 1995;9(1):44-54.
1994: Adriaan P IJzerman; E M van der Wenden; Jacobien K Von Frijtag Drabbe Künzel; R A Mathôt; Meindert Danhof; P A Borea; K Varani
Partial agonism of theophylline-7-riboside on adenosine receptors.
Naunyn-Schmiedeberg's archives of pharmacology 1994;350(6):638-45.
1994: A Van Der Bent; Adriaan P IJzerman; Willem Soudijn
Molecular modelling of CCK-A receptors.
Drug design and discovery 1994;12(2):129-48.
1994: Hubertus Irth; Anne-Marie Cleton; R A Mathôt; Meindert Danhof; Adriaan P IJzerman; Ubbo R Tjaden; Jan van der Greef
Liquid chromatographic determination of the adenosine receptor agonist CGS 21680 in blood using on-line solid-phase extraction on a phenylboronic acid support and fluorescence detection.
Journal of chromatography. B, Biomedical applications 1994;658(1):207-12.
1994: R A Mathôt; B C Van den Aarsen; J K von Frijtag Drabble Künzel; Meindert Danhof; Adriaan P IJzerman
Assessment of the enantiomeric purity of R- and S-N6-phenylisopropyladenosine (PIA): implications for adenosine receptor subclassification.
Naunyn-Schmiedeberg's archives of pharmacology 1994;350(1):109-12.
1994: Adriaan P IJzerman; E M van der Wenden; P J van Galen; Kenneth Alan Jacobson
Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor.
European journal of pharmacology 1994;268(1):95-104.
1994: A M van Rhee; M P van der Heijden; Margot W Beukers; Adriaan P IJzerman; Willem Soudijn; Peter Nickel
Novel competitive antagonists for P2 purinoceptors.
European journal of pharmacology 1994;268(1):1-7.
1994: P J van Galen; A H van Bergen; C Gallo-Rodriguez; Neli Melman; ME Olah; Adriaan P IJzerman; Gary L Stiles; Kenneth Alan Jacobson
A binding site model and structure-activity relationships for the rat A3 adenosine receptor.
Molecular pharmacology 1994;45(6):1101-11.
1994: W Kuipers; Ineke van Wijngaarden; Adriaan P IJzerman
A model of the serotonin 5-HT1A receptor: agonist and antagonist binding sites.
Drug design and discovery 1994;11(3):231-49.
1994: R A Mathôt; EA van Schaick; MW Langemeijer; Willem Soudijn; Douwe D Breimer; Adriaan P IJzerman; Meindert Danhof
Pharmacokinetic-pharmacodynamic relationship of the cardiovascular effects of adenosine A1 receptor agonist N6-cyclopentyladenosine in the rat.
The Journal of pharmacology and experimental therapeutics 1994;268(2):616-24.
1994: Margot W Beukers; C J Kerkhof; Adriaan P IJzerman; Willem Soudijn
Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016.
European journal of pharmacology 1994;266(1):57-62.
1993: Margot W Beukers; I M Pirovano; A van Weert; C J Kerkhof; Adriaan P IJzerman; Willem Soudijn
Characterization of ecto-ATPase on human blood cells. A physiological role in platelet aggregation?
Biochemical pharmacology 1993;46(11):1959-66.
1993: R A Mathôt; S Appel; EA van Schaick; Willem Soudijn; Adriaan P IJzerman; Meindert Danhof
High-performance liquid chromatography of the adenosine A1 agonist N6-cyclopentyladenosine and the A1 antagonist 8-cyclopentyltheophylline and its application in a pharmacokinetic study in rats.
Journal of chromatography 1993;620(1):113-20.
1993: A M van Rhee; E C van Winden; J Fred Nagelkerke; Hans J G M De Bont; Adriaan P IJzerman; Willem Soudijn
Binding of the radioligand [35S]adenosine 5'-O-(2-thiodiphosphate) and intracellular calcium response in rat liver parenchymal cells.
Biochemical pharmacology 1993;45(4):801-7.
1992: A Van der Bent; Antonius Marinus ter Laak; Adriaan P IJzerman; Willem Soudijn
Molecular modelling of asperlicin derived cholecystokinin A receptor antagonists.
European journal of pharmacology 1992;226(4):327-34.
1992: Adriaan P IJzerman; M Kruidering; A van Weert; H van Belle; C Janssen
[3H]R75231--a new radioligand for the nitrobenzylthioinosine sensitive nucleoside transport proteins. Characterization of (+/-)-[3H]R75231 binding to calf lung membranes, stereospecificity of its two stereoisomers, and comparison with [3H]nitrobenzylthioinosine binding.
Naunyn-Schmiedeberg's archives of pharmacology 1992;345(5):558-63.
1992: A van der Bent; A G Blommaert; C T Melman; Adriaan P IJzerman; Ineke van Wijngaarden; Willem Soudijn
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
Journal of medicinal chemistry 1992;35(6):1042-9.
1992: E M van der Wenden; Adriaan P IJzerman; Willem Soudijn
A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor.
Journal of medicinal chemistry 1992;35(4):629-35.
1992: Adriaan P IJzerman; C T Melman
Chemical modification of cholecystokinin-A receptors in rat pancreatic membranes.
European journal of biochemistry / FEBS 1992;203(3):521-6.
1992: A Garritsen; Margot W Beukers; Adriaan P IJzerman; E J Cragoe; Willem Soudijn
The mode of interaction of amiloride and some of its analogues with the adenosine A1 receptor.
Neurochemistry international 1992;20(2):207-13.
1992: Adriaan P IJzerman; P J Van Galen; Kenneth Alan Jacobson
Molecular modeling of adenosine receptors. I. The ligand binding site on the A1 receptor.
Drug design and discovery 1992;9(1):49-67.
1991: E M Van der Wenden; P J Van Galen; Adriaan P IJzerman; Willem Soudijn
Mapping the xanthine C8-region of the adenosine A1 receptor with computer graphics.
European journal of pharmacology 1991;206(4):315-23.
1991: P J van Galen; P Nissen; Ineke van Wijngaarden; Adriaan P IJzerman; Willem Soudijn
1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Journal of medicinal chemistry 1991;34(3):1202-6.
1991: Adriaan P IJzerman; A Voorschuur; M Kruidering; I M Pirovano; H Van Belle; C Janssen
Radioligand binding studies on the nucleoside transport protein.
Advances in experimental medicine and biology 1991;309A():411-4.
1991: A Garritsen; Adriaan P IJzerman; Martin Tulp; E J Cragoe; Willem Soudijn
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.
Journal of receptor research 1991;11(6):891-907.
1990: I M Pirovano; H Van Belle; Adriaan P IJzerman
Inhibition of nucleoside uptake in human erythrocytes by a new series of compounds related to lidoflazine and mioflazine.
European journal of pharmacology 1990;189(6):419-22.
1990: Adriaan P IJzerman; A H Voorschuur
The relationship between ionization and affinity of nucleoside transport inhibitors.
Naunyn-Schmiedeberg's archives of pharmacology 1990;342(3):336-41.
1990: A Garritsen; Adriaan P IJzerman; Margot W Beukers; Willem Soudijn
Chemical modification of adenosine A1 receptors. Implications for the interaction with R-PIA, DPCPX and amiloride.
Biochemical pharmacology 1990;40(4):835-42.
1990: A Garritsen; Adriaan P IJzerman; Margot W Beukers; E J Cragoe; Willem Soudijn
Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain.
Biochemical pharmacology 1990;40(4):827-34.
1990: P J van Galen; Herman van Vlijmen; Adriaan P IJzerman; Willem Soudijn
A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties.
Journal of medicinal chemistry 1990;33(6):1708-13.
1989: Adriaan P IJzerman; K H Thedinga; A F Custers; B Hoos; H Van Belle
Inhibition of nucleoside transport by a new series of compounds related to lidoflazine and mioflazine.
European journal of pharmacology 1989;172(3):273-81.
1989: Herman van Vlijmen; Adriaan P IJzerman
Molecular modeling of a putative antagonist binding site on helix III of the beta-adrenoceptor.
Journal of computer-aided molecular design 1989;3(2):165-74.
1989: I M Pirovano; Adriaan P IJzerman; P J Van Galen; Willem Soudijn
Influence of the molecular structure of N6-(omega-aminoalkyl)adenosines on adenosine receptor affinity and intrinsic activity.
European journal of pharmacology 1989;172(2):185-93.
1989: P J Van Galen; F J Leusen; Adriaan P IJzerman; Willem Soudijn
Mapping the N6-region of the adenosine A1 receptor with computer graphics.
European journal of pharmacology 1989;172(1):19-27.
1989: Adriaan P IJzerman; G J Menkveld; K H Thedinga
A refined method for the photoaffinity labelling of the nitrobenzylthioinosine-sensitive nucleoside transport protein: application to cell membranes of calf lung tissue.
Biochimica et biophysica acta 1989;979(2):153-6.
1989: A Garritsen; Adriaan P IJzerman; Willem Soudijn
Adenosine-A1 receptors are not coupled to Ca2+ uptake in rat brain synaptosomes.
Biochemical pharmacology 1989;38(4):693-5.
1988: Adriaan P IJzerman
Limiting solubilities and ionization constants of sparingly soluble compounds: determination from aqueous potentiometric titration data only.
Pharmaceutical research 1988;5(12):772-5.
1988: Adriaan P IJzerman; Herman van Vlijmen
A molecular graphics study exploring a putative ligand binding site of the beta-adrenoceptor.
Journal of computer-aided molecular design 1988;2(1):43-53.
1988: A Garritsen; Adriaan P IJzerman; Willem Soudijn
[3H]batrachotoxinin-A 20-alpha-benzoate binding to sodium channels in rat brain: sensitivity to tetrodotoxin and divalent cations.
European journal of pharmacology 1988;145(3):261-6.
1987: Adriaan P IJzerman; A Nagesser; A Garritsen
The membrane stabilizing activity of beta-adrenoceptor ligands. Quantitative evaluation of the interaction of phenoxypropanolamines with the [3H]batrachotoxinin A 20-alpha-benzoate binding site on voltage-sensitive sodium channels in rat brain.
Biochemical pharmacology 1987;36(24):4239-44.
1987: P J van Galen; Adriaan P IJzerman; Willem Soudijn
Adenosine derivatives with N6-alkyl, -alkylamine or -alkyladenosine substituents as probes for the A1-receptor.
FEBS letters 1987;223(1):197-201.