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Erik Falch

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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.
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.
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.

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All Publications

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.
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.
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.
2001: U S Sørensen; Erik Falch; Tine B Stensbøl; Jerzy W Jaroszewski; Ulf Madsen; Povl Krogsgaard-Larsen
Structural determinants for AMPA agonist activity of aryl or heteroaryl substituted AMPA analogues. Synthesis and pharmacology.
Archiv der Pharmazie 2001;334(2):62-8.
2000: U S Sørensen; Erik Falch; Povl Krogsgaard-Larsen
A novel route to 5-substituted 3-isoxazolols. Cyclization of N, O-DiBoc beta-keto hydroxamic acids synthesized via acyl Meldrum's acids.
The Journal of organic chemistry 2000;65(4):1003-7.
1999: Erik Falch; Jens Perregaard; B FrŁlund; B SŁkilde; Anders Buur; L M Hansen; Karla Frydenvang; Lotte Brehm; Tina Bolvig; Orla M Larsson; Connie Sanchez; H White; Arne Schousboe; Povl Krogsgaard-Larsen
Selective inhibitors of glial GABA uptake: synthesis, absolute stereochemistry, and pharmacology of the enantiomers of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO) and analogues.
Journal of medicinal chemistry 1999;42(26):5402-14.
1999: Tina Bolvig; Orla M Larsson; Darryl S Pickering; N Nelson; Erik Falch; Povl Krogsgaard-Larsen; Arne Schousboe
Action of bicyclic isoxazole GABA analogues on GABA transporters and its relation to anticonvulsant activity.
European journal of pharmacology 1999;375(1-3):367-74.
1998: Erik Falch; Lotte Brehm; Ivan Mikkelsen; Tommy N Johansen; N Skjaerbaek; Birgitte Nielsen; Tine B Stensbøl; Bjarke Ebert; Povl Krogsgaard-Larsen
Heteroaryl analogues of AMPA. 2. Synthesis, absolute stereochemistry, photochemistry, and structure-activity relationships.
Journal of medicinal chemistry 1998;41(14):2513-23.
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.
1998: N Skjaerbaek; Lotte Brehm; Tommy N Johansen; L M Hansen; Birgitte Nielsen; Bjarke Ebert; Karina Krøjer Søby; Tine B Stensbøl; Erik Falch; Povl Krogsgaard-Larsen
Aryl and cycloalkyl analogues of AMPA: synthetic, pharmacological and stereochemical aspects.
Bioorganic & medicinal chemistry 1998;6(1):119-31.
1997: Tommy N Johansen; Bjarke Ebert; Erik Falch; Povl Krogsgaard-Larsen
AMPA receptor agonists: resolution, configurational assignment, and pharmacology of (+)-(S)- and (-)-(R)-2-amino-3-[3-hydroxy-5-(2-pyridyl)-isoxazol-4-yl]-propionic acid (2-Py-AMPA).
Chirality 1997;9(3):274-80.
1996: Hans Bräuner-Osborne; Bjarke Ebert; Mark R Brann; Erik Falch; Povl Krogsgaard-Larsen
Functional partial agonism at cloned human muscarinic acetylcholine receptors.
European journal of pharmacology 1996;313(1-2):145-50.
1996: B Søkilde; I Mikkelsen; Tine B Stensbøl; B Andersen; S Ebdrup; Povl Krogsgaard-Larsen; Erik Falch
Analogues of carbacholine: synthesis and relationship between structure and affinity for muscarinic and nicotinic acetylcholine receptors.
Archiv der Pharmazie 1996;329(2):95-104.
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: Hans Bräuner-Osborne; Bjarke Ebert; Mark R Brann; Erik Falch; Povl Krogsgaard-Larsen
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.
Journal of medicinal chemistry 1995;38(12):2188-95.
1993: H White; J Hunt; HH Wolf; E A Swinyard; Erik Falch; P Krogsgaard-Larsen; A Schousboe
Anticonvulsant activity of the gamma-aminobutyric acid uptake inhibitor N-4,4-diphenyl-3-butenyl-4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol .
European journal of pharmacology 1993;236(1):147-9.
1993: A Lagersted; Erik Falch; Bjarke Ebert; Povl Krogsgaard-Larsen
Conformational aspects of the muscarinic receptor interactions of bicyclic isoxazole ester bioisosteres of arecoline.
Drug design and discovery 1993;9(3-4):237-50.
1992: U Kristiansen; A Hedegaard; C Herdeis; T M Lund; Birgitte Nielsen; J J Hansen; Erik Falch; H Hjeds; Povl Krogsgaard-Larsen
Hydroxylated analogues of 5-aminovaleric acid as 4-aminobutyric acidB receptor antagonists: stereostructure-activity relationships.
Journal of neurochemistry 1992;58(3):1150-9.
1991: U Kristiansen; J D Lambert; Erik Falch; Povl Krogsgaard-Larsen
Electrophysiological studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones.
British journal of pharmacology 1991;104(1):85-90.
1989: Erik Falch; Povl Krogsgaard-Larsen
GABA uptake inhibitors containing mono- and diarylmethoxyalkyl N-substituents.
Drug design and delivery 1989;4(3):205-15.
1988: P Sauerberg; Erik Falch; E Meier; H L Lembøl; Povl Krogsgaard-Larsen
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Journal of medicinal chemistry 1988;31(7):1312-6.
1988: O M Larsson; Erik Falch; P Krogsgaard-Larsen; A Schousboe
Kinetic characterization of inhibition of gamma-aminobutyric acid uptake into cultured neurons and astrocytes by 4,4-diphenyl-3-butenyl derivatives of nipecotic acid and guvacine.
Journal of neurochemistry 1988;50(3):818-23.
1988: Povl Krogsgaard-Larsen; Erik Falch; P Sauerberg; S B Freedman; H L Lembøl; E Meier
Bioisosteres of arecoline as novel CNS-active muscarinic agonists.
Trends in pharmacological sciences 1988;Suppl():69-74.
1987: Erik Falch; B S Meldrum; Povl Krogsgaard-Larsen
GABA uptake inhibitors. Synthesis and effects on audiogenic seizures of ester prodrugs of nipecotic acid, guvacine and cis-4-hydroxynipecotic acid.
Drug design and delivery 1987;2(1):9-21.
1987: J R Byberg; I M Labouta; Erik Falch; H Hjeds; Povl Krogsgaard-Larsen; D R Curtis; B D Gynther
Synthesis and biological activity of a GABAA agonist which has no effect on benzodiazepine binding and of structurally related glycine antagonists.
Drug design and delivery 1987;1(4):261-74.
1987: Povl Krogsgaard-Larsen; Erik Falch; O M Larsson; A Schousboe
GABA uptake inhibitors: relevance to antiepileptic drug research.
Epilepsy research 1987;1(2):77-93.
1986: P Sauerberg; B Fjalland; J J Larsen; T Bach-Lauritsen; Erik Falch; Povl Krogsgaard-Larsen
Pharmacological profile of a novel class of muscarinic acetylcholine receptor agonists.
European journal of pharmacology 1986;130(1-2):125-31.
1986: Erik Falch; A Hedegaard; L Nielsen; B R Jensen; H Hjeds; Povl Krogsgaard-Larsen
Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations.
Journal of neurochemistry 1986;47(3):898-903.
1986: P Sauerberg; J J Larsen; Erik Falch; Povl Krogsgaard-Larsen
A novel class of conformationally restricted heterocyclic muscarinic agonists.
Journal of medicinal chemistry 1986;29(6):1004-9.
1986: Lotte Brehm; Povl Krogsgaard-Larsen; K Schaumburg; J S Johansen; Erik Falch; D R Curtis
Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions.
Journal of medicinal chemistry 1986;29(2):224-9.
1986: A Buur; H Bundgaard; Erik Falch
Prodrugs of 5-fluorouracil. VII. Hydrolysis kinetics and physicochemical properties of N-ethoxy- and N-phenoxycarbonyloxymethyl derivatives of 5-fluorouracil.
Acta pharmaceutica Suecica 1986;23(4):205-16.
1985: P Krogsgaard-Larsen; L Nielsen; Erik Falch; D R Curtis
GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol.
Journal of medicinal chemistry 1985;28(11):1612-7.
1985: Erik Falch; P Jacobsen; Povl Krogsgaard-Larsen; D R Curtis
GABA-mimetic activity and effects on diazepam binding of aminosulphonic acids structurally related to piperidine-4-sulphonic acid.
Journal of neurochemistry 1985;44(1):68-75.
1985: Povl Krogsgaard-Larsen; Erik Falch; H Hjeds
Heterocyclic analogues of GABA: chemistry, molecular pharmacology and therapeutic aspects.
Progress in medicinal chemistry 1985;22():67-120.
1983: Povl Krogsgaard-Larsen; H Mikkelsen; P Jacobsen; Erik Falch; D R Curtis; M J Peet; J D Leah
4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity.
Journal of medicinal chemistry 1983;26(6):895-900.
1983: Povl Krogsgaard-Larsen; Erik Falch; M J Peet; J D Leah; D R Curtis
Molecular pharmacology of the GABA receptors and GABA agonists.
Advances in biochemical psychopharmacology 1983;37():1-13.
1982: P Jacobsen; I M Labouta; K Schaumburg; Erik Falch; Povl Krogsgaard-Larsen
Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors.
Journal of medicinal chemistry 1982;25(10):1157-62.
1980: P Krogsgaard-Larsen; Erik Falch; A Schousboe; D R Curtis; D Lodge
Piperidine-4-sulphonic acid, a new specific GABA agonist.
Journal of neurochemistry 1980;34(3):756-9.