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Bente Frølund

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Anders A Jensen; Jacob Krall; Povl Krogsgaard-Larsen; Martin H F Pedersen; Niels Plath; Tine B Stensbøl; Petrine Wellendorph; David E Gloriam; Vignir Isberg; Bente Frølund
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.
Jette G Petersen; Thomas Balle; Rikke Bergmann; Karla Frydenvang; Anders A Jensen; Charlotte G Jørgensen; Jan Kehler; Jesper Kristensen; Uffe Kristiansen; Henriette A Møller; Birgitte Nielsen; Bente Frølund
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
Christine A Ussing; Philip K Ahring; Bente Frølund; Michael Gajhede; Camilla P Hansen; Anders A Jensen; Jette S Kastrup; Elsebet Ø Nielsen; Jette G Petersen; Line A H Rohde; Thomas Balle
Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists.

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All Publications

2013: Anders A Jensen; Jacob Krall; Povl Krogsgaard-Larsen; Martin H F Pedersen; Niels Plath; Tine B Stensbøl; Petrine Wellendorph; David E Gloriam; Vignir Isberg; Bente Frølund
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.
Journal of medicinal chemistry 2013;56(3):1211-27.
2013: Jette G Petersen; Thomas Balle; Rikke Bergmann; Karla Frydenvang; Anders A Jensen; Charlotte G Jørgensen; Jan Kehler; Jesper Kristensen; Uffe Kristiansen; Henriette A Møller; Birgitte Nielsen; Bente Frølund
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.
Journal of medicinal chemistry 2013;56(3):993-1006.
2013: Christine A Ussing; Philip K Ahring; Bente Frølund; Michael Gajhede; Camilla P Hansen; Anders A Jensen; Jette S Kastrup; Elsebet Ø Nielsen; Jette G Petersen; Line A H Rohde; Thomas Balle
Synthesis, pharmacology, and biostructural characterization of novel α4β2 nicotinic acetylcholine receptor agonists.
Journal of medicinal chemistry 2013;56(3):940-51.
2012: Nathan Absalom; Tina Bay; Hans Bräuner-Osborne; Mary Chebib; Rasmus P Clausen; Laura F Eghorn; Bente Frølund; Nasiara Karim; Gitte M Knudsen; Jesper V Olsen; Inge S Villumsen; Petrine Wellendorph
α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB).
Proceedings of the National Academy of Sciences of the United States of America 2012;109(33):13404-9.
2011: Tommy Sander; Bente Frølund; Anne Techau Bruun; Ivaylo Ivanov; James Andrew McCammon; Thomas Balle
New insights into the GABA(A) receptor structure and orthosteric ligand binding: receptor modeling guided by experimental data.
Proteins 2011;79(5):1458-77.
2011: Charlotte G Jørgensen; Bente Frølund; Jan Kehler; Anders A Jensen
Discovery of benzamide analogues as a novel class of 5-HT₃ receptor agonists.
ChemMedChem 2011;6(4):725-36.
2010: Petrine Wellendorph; Signe Høg; Paola Sabbatini; Martin H F Pedersen; Lars Martiny; Gitte M Knudsen; Bente Frølund; Rasmus P Clausen; Hans Bräuner-Osborne
Novel radioiodinated {gamma}-hydroxybutyric acid analogues for radiolabeling and Photolinking of high-affinity {gamma}-hydroxybutyric acid binding sites.
The Journal of pharmacology and experimental therapeutics 2010;335(2):458-64.
2010: Paola Sabbatini; Petrine Wellendorph; Signe Høg; Martin H F Pedersen; Hans Bräuner-Osborne; Lars Martiny; Bente Frølund; Rasmus P Clausen
Design, synthesis, and in vitro pharmacology of new radiolabeled gamma-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity gamma-hydroxybutyric acid binding sites.
Journal of medicinal chemistry 2010;53(17):6506-10.
2010: Henriette A Møller; Tommy Sander; Jesper L Kristensen; Birgitte Nielsen; Jacob Krall; Marianne L Bergmann; Bolette Christiansen; Thomas Balle; Anders A Jensen; Bente Frølund
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.
Journal of medicinal chemistry 2010;53(8):3417-21.
2009: Camilla P Hansen; Anders A Jensen; Thomas Balle; Klaus Bitsch-Jensen; Mohamud M Hassan; Tommy Liljefors; Bente Frølund
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Bioorganic & medicinal chemistry letters 2009;19(1):87-91.
2008: Signe Høg; Petrine Wellendorph; Birgitte Nielsen; Karla Frydenvang; Ivar F Dahl; Hans Bräuner-Osborne; Lotte Brehm; Bente Frølund; Rasmus P Clausen
Novel high-affinity and selective biaromatic 4-substituted gamma-hydroxybutyric acid (GHB) analogues as GHB ligands: design, synthesis, and binding studies.
Journal of medicinal chemistry 2008;51(24):8088-95.
2008: Camilla P Hansen; Anders A Jensen; Jeppe K Christensen; Thomas Balle; Tommy Liljefors; Bente Frølund
Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist.
Journal of medicinal chemistry 2008;51(23):7380-95.
2008: Mie Larsen; Birger Brodin Larsen; Bente Frølund; Carsten Uhd Nielsen
Transport of amino acids and GABA analogues via the human proton-coupled amino acid transporter, hPAT1: characterization of conditions for affinity and transport experiments in Caco-2 cells.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 2008;35(1-2):86-95.
2008: Misty Smith; Gerald W Saunders; Rasmus P Clausen; Bente Frølund; Povl Krogsgaard-Larsen; Orla M Larsson; Arne Schousboe; Karen S Wilcox; H White
Inhibition of the betaine-GABA transporter (mGAT2/BGT-1) modulates spontaneous electrographic bursting in the medial entorhinal cortex (mEC).
Epilepsy research 2008;79(1):6-13.
2007: Christian Madsen; Anders A Jensen; Tommy Liljefors; Uffe Kristiansen; Birgitte Nielsen; Camilla P Hansen; Mogens Larsen; Bjarke Ebert; Benny Bang-Andersen; Povl Krogsgaard-Larsen; Bente Frølund
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
Journal of medicinal chemistry 2007;50(17):4147-61.
2007: Rüdiger Faust; Peter J Garratt; Maria Angeles Trujillo Pérez; Vincent J-D Piccio; Christian Madsen; Ane Stenstrøm; Bente Frølund; Kathryn Davidson; Muy-Teck Teh; David Sugden
7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.
Bioorganic & medicinal chemistry 2007;15(13):4543-51.
2007: Bente Frølund; Lars S Jensen; Signe I Storustovu; Tine B Stensbøl; Bjarke Ebert; Jan Kehler; Povl Krogsgaard-Larsen; Tommy Liljefors
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
Journal of medicinal chemistry 2007;50(8):1988-92.
2007: Henrik T Vestergaard; Carolina Cannillo; Bente Frølund; Uffe Kristiansen
Differences in kinetics of structurally related competitive GABA(A) receptor antagonists.
Neuropharmacology 2007;52(3):873-82.
2006: Rasmus P Clausen; Bente Frølund; Orla M Larsson; Arne Schousboe; Povl Krogsgaard-Larsen; H White
A novel selective gamma-aminobutyric acid transport inhibitor demonstrates a functional role for GABA transporter subtype GAT2/BGT-1 in the CNS.
Neurochemistry international 2006;48(6-7):637-42.
2006: Dorte Krehan; Signe I Storustovu; Tommy Liljefors; Bjarke Ebert; Birgitte Nielsen; Povl Krogsgaard-Larsen; Bente Frølund
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Journal of medicinal chemistry 2006;49(4):1388-96.
2006: Rasmus P Clausen; Karsten Madsen; Orla M Larsson; Bente Frølund; Povl Krogsgaard-Larsen; Arne Schousboe
Structure-activity relationship and pharmacology of gamma-aminobutyric acid (GABA) transport inhibitors.
Advances in pharmacology (San Diego, Calif.) 2006;54():265-84.
2006: Povl Krogsgaard-Larsen; Bente Frølund; Tommy Liljefors
GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.
Advances in pharmacology (San Diego, Calif.) 2006;54():53-71.
2006: Signe Høg; Jeremy R Greenwood; Karsten B Madsen; Orla M Larsson; Bente Frølund; Arne Schousboe; Povl Krogsgaard-Larsen; Rasmus P Clausen
Structure-activity relationships of selective GABA uptake inhibitors.
Current topics in medicinal chemistry 2006;6(17):1861-82.
2005: Petrine Wellendorph; Signe Høg; Jeremy R Greenwood; Anne de Lichtenberg; Birgitte Nielsen; Bente Frølund; Lotte Brehm; Rasmus P Clausen; Hans Bräuner-Osborne
Novel cyclic gamma-hydroxybutyrate (GHB) analogs with high affinity and stereoselectivity of binding to GHB sites in rat brain.
The Journal of pharmacology and experimental therapeutics 2005;315(1):346-51.
2005: Bente Frølund; Jeremy R Greenwood; Mai Marie Holm; Jan Egebjerg; Ulf Madsen; Birgitte Nielsen; Hans Bräuner-Osborne; Tine B Stensbøl; Povl Krogsgaard-Larsen
Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: synthesis, modelling and molecular pharmacology.
Bioorganic & medicinal chemistry 2005;13(18):5391-8.
2005: Anders A Jensen; Bente Frølund; Tommy Liljefors; Povl Krogsgaard-Larsen
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Journal of medicinal chemistry 2005;48(15):4705-45.
2005: Rasmus P Clausen; Ejner K Moltzen; Jens Perregaard; Sibylle M Lenz; Connie Sanchez; Erik Falch; Bente Frølund; Tina Bolvig; Alan Sarup; Orla M Larsson; Arne Schousboe; Povl Krogsgaard-Larsen
Selective inhibitors of GABA uptake: synthesis and molecular pharmacology of 4-N-methylamino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol analogues.
Bioorganic & medicinal chemistry 2005;13(3):895-908.
2005: H White; William P Watson; Suzanne L Hansen; Scott Slough; Jens Perregaard; Alan Sarup; Tina Bolvig; Gitte Petersen; Orla M Larsson; Rasmus P Clausen; Bente Frølund; Erik Falch; Povl Krogsgaard-Larsen; Arne Schousboe
First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.
The Journal of pharmacology and experimental therapeutics 2005;312(2):866-74.
2005: Bente Frølund; Lars S Jensen; Luca Guandalini; Carolina Canillo; Henrik T Vestergaard; Uffe Kristiansen; Birgitte Nielsen; Tine B Stensbøl; Christian Madsen; Povl Krogsgaard-Larsen; Tommy Liljefors
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Journal of medicinal chemistry 2005;48(2):427-39.
2004: Povl Krogsgaard-Larsen; Bente Frølund; Tommy Liljefors; Bjarke Ebert
GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.
Biochemical pharmacology 2004;68(8):1573-80.
2004: Anders A Jensen; Ivan Mikkelsen; Bente Frølund; Karla Frydenvang; Lotte Brehm; Jerzy W Jaroszewski; Hans Bräuner-Osborne; Erik Falch; Povl Krogsgaard-Larsen
Carbamoylcholine homologs: synthesis and pharmacology at nicotinic acetylcholine receptors.
European journal of pharmacology 2004;497(2):125-37.
2004: Martin Mortensen; Uffe Kristiansen; Bjarke Ebert; Bente Frølund; Povl Krogsgaard-Larsen; Trevor G Smart
Activation of single heteromeric GABA(A) receptor ion channels by full and partial agonists.
The Journal of physiology 2004;557(Pt 2):389-413.
2003: Dorte Krehan; Bente Frølund; Bjarke Ebert; Birgitte Nielsen; Povl Krogsgaard-Larsen; Graham A R Johnston; Mary Chebib
Aza-THIP and related analogues of THIP as GABA C antagonists.
Bioorganic & medicinal chemistry 2003;11(23):4891-6.
2003: Anders A Jensen; Ivan Mikkelsen; Bente Frølund; Hans Bräuner-Osborne; Erik Falch; Povl Krogsgaard-Larsen
Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors.
Molecular pharmacology 2003;64(4):865-75.
2003: Alan Sarup; Orla M Larsson; Tina Bolvig; Bente Frølund; Povl Krogsgaard-Larsen; Arne Schousboe
Effects of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazol (exo-THPO) and its N-substituted analogs on GABA transport in cultured neurons and astrocytes and by the four cloned mouse GABA transporters.
Neurochemistry international 2003;43(4-5):445-51.
2003: Dorte Krehan; Bente Frølund; Povl Krogsgaard-Larsen; Jan Kehler; Graham A R Johnston; Mary Chebib
Phosphinic, phosphonic and seleninic acid bioisosteres of isonipecotic acid as novel and selective GABA(C) receptor antagonists.
Neurochemistry international 2003;42(7):561-5.
2003: Bente Frølund; Lena Tagmose; Anne T Jørgensen; Uffe Kristiansen; Tine B Stensbøl; Tommy Liljefors; Povl Krogsgaard-Larsen
Design and synthesis of a new series of 4-alkylated 3-isoxazolol GABA A antagonists.
European journal of medicinal chemistry 2003;38(4):447-9.
2002: Martin Mortensen; Bente Frølund; Anne T Jørgensen; Tommy Liljefors; Povl Krogsgaard-Larsen; Bjarke Ebert
Activity of novel 4-PIOL analogues at human alpha 1 beta 2 gamma 2S GABA(A) receptors--correlation with hydrophobicity.
European journal of pharmacology 2002;451(2):125-32.
2002: Bjarke Ebert; S i Storustovu; Martin Mortensen; Bente Frølund
Characterization of GABA(A) receptor ligands in the rat cortical wedge preparation: evidence for action at extrasynaptic receptors?
British journal of pharmacology 2002;137(1):1-8.
2002: Bente Frølund; Bjarke Ebert; Uffe Kristiansen; Tommy Liljefors; Povl Krogsgaard-Larsen
GABA(A) receptor ligands and their therapeutic potentials.
Current topics in medicinal chemistry 2002;2(8):817-32.
2002: H White; Alan Sarup; Tina Bolvig; Anders Skov Kristensen; Gitte Petersen; Nathan Nelson; Darryl S Pickering; Orla M Larsson; Bente Frølund; Povl Krogsgaard-Larsen; Arne Schousboe
Correlation between anticonvulsant activity and inhibitory action on glial gamma-aminobutyric acid uptake of the highly selective mouse gamma-aminobutyric acid transporter 1 inhibitor 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and its N-alkylated analogs.
The Journal of pharmacology and experimental therapeutics 2002;302(2):636-44.
2002: Bente Frølund; Anne T Jørgensen; Lena Tagmose; Tine B Stensbøl; Henrik T Vestergaard; Christine Engblom; Uffe Kristiansen; Connie Sanchez; Povl Krogsgaard-Larsen; Tommy Liljefors
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Journal of medicinal chemistry 2002;45(12):2454-68.
2002: Povl Krogsgaard-Larsen; Bente Frølund; Tommy Liljefors
Specific GABA(A) agonists and partial agonists.
Chemical record (New York, N.Y.) 2002;2(6):419-30.
2000: Bente Frølund; Lena Tagmose; Tommy Liljefors; Tine B Stensbøl; C Engblom; Uffe Kristiansen; Povl Krogsgaard-Larsen
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Journal of medicinal chemistry 2000;43(26):4930-3.
2000: Povl Krogsgaard-Larsen; Bente Frølund; Karla Frydenvang
GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects.
Current pharmaceutical design 2000;6(12):1193-209.
1998: Povl Krogsgaard-Larsen; Bente Frølund; Erik Falch
Inhibitors of gamma-aminobutyric acid transport as experimental tools and therapeutic agents.
Methods in enzymology 1998;296():165-75.
1997: L Matzen; Bjarke Ebert; Tine B Stensbøl; Bente Frølund; Jerzy W Jaroszewski; Povl Krogsgaard-Larsen
Bioisosterically modified dipeptide excitatory amino acid receptor antagonists containing 3-oxygenated isothiazole ring systems.
Bioorganic & medicinal chemistry 1997;5(8):1569-75.
1997: L Matzen; A Engesgaard; Bjarke Ebert; Michael Didriksen; Bente Frølund; Povl Krogsgaard-Larsen; Jerzy W Jaroszewski
AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.
Journal of medicinal chemistry 1997;40(4):520-7.
1996: Jerzy W Jaroszewski; L Matzen; Bente Frølund; Povl Krogsgaard-Larsen
Neuroactive polyamine wasp toxins: nuclear magnetic resonance spectroscopic analysis of the protolytic properties of philanthotoxin-343.
Journal of medicinal chemistry 1996;39(2):515-21.
1995: Bente Frølund; U Kristiansen; Lotte Brehm; A B Hansen; Povl Krogsgaard-Larsen; Erik Falch
Partial GABAA receptor agonists. Synthesis and in vitro pharmacology of a series of nonannulated analogs of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol.
Journal of medicinal chemistry 1995;38(17):3287-96.
1995: Bente Frølund; L Jeppesen; Povl Krogsgaard-Larsen; J J Hansen
GABAA agonists: resolution and pharmacology of (+)- and (-)-isoguvacine oxide.
Chirality 1995;7(6):434-8.
1994: Povl Krogsgaard-Larsen; Bente Frølund; Flemming Steen Jørgensen; A Schousboe
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
Journal of medicinal chemistry 1994;37(16):2489-505.