title: Thienyl-GABA derivatives as specific baclofen agonists in the rat and cat spinal cord in vivo.
abstract: The depression of the amplitude of extracellularly recorded monosynaptic excitatory field potentials in the lumbar spinal cord of pentobarbitone anaesthetised rats and cats by three thienyl derivatives of GABA: 4-amino-3-(2-thienyl)-butanoic acid; 4-amino-3-(2-thienyl-5-methyl)-butanoic acid and 4-amino-3-(2-thienyl-5-chloro)-butanoic acid was reversibly blocked by the (-)-baclofen antagonist 3-aminopropyl-diethoxymethyl-phosphinic acid (CGP 35348). These compounds, of which the most potent, the 5-chloro derivative, was weaker than (-)-baclofen, thus activate baclofen receptors in the cat and rat spinal cord.
authors.affiliation: Division of Neuroscience, John Curtin School of Medical Research, Canberra, ACT Australia.
authors.forename: G
authors.initials: G
authors.lastname: Lacey
authors.forename: P
authors.initials: P
authors.lastname: Berthelot
authors.forename: C
authors.initials: C
authors.lastname: Vaccher
authors.forename: N
authors.initials: N
authors.lastname: Flouquet
authors.forename: M P
authors.initials: MP
authors.lastname: Vaccher
authors.forename: M
authors.initials: M
authors.lastname: Debaert
authors.forename: D R
authors.initials: DR
authors.lastname: Curtis
mesh_terms: D000818:Animals; D001418:Baclofen / Q000494:pharmacology*; D002415:Cats; D004586:Electrophoresis; D005071:Evoked Potentials / Q000187:drug effects; D058787:GABA-A Receptor Antagonists; D009943:Organophosphorus Compounds / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D018079:Receptors, GABA / Q000187:drug effects; D018080:Receptors, GABA-B / Q000187:drug effects; D013116:Spinal Cord / Q000187:drug effects*; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*
chemical_list: D058787:GABA-A Receptor Antagonists; D009943:Organophosphorus Compounds; D018079:Receptors, GABA; D018080:Receptors, GABA-B; D005680:gamma-Aminobutyric Acid; C066430:CGP 35348; D001418:Baclofen