title: CGP 55845A: a potent antagonist of GABAB receptors in the CA1 region of rat hippocampus.
abstract: The new GABAB receptor antagonist CGP 55845A was tested on pre- and post-synaptic GABAB receptors in the hippocampus. CGP 55845A (1 microM) blocked (-)-baclofen (5-10 microM)-induced postsynaptic hyperpolarization and depression of evoked IPSPs and EPSPs. It also blocked three physiological consequences of GABAB receptor activation: the late IPSP, paired-pulse depression of IPSCs, and heterosynaptic depression of EPSPs. Therefore, CGP 55845A is an antagonist at pre- and post-synaptic GABAB receptors in the hippocampus and is approximately three orders of magnitude more potent than previously described GABAB receptor antagonists.
authors.affiliation: Department of Pharmacology, Medical School, University of Birmingham, Edgbaston, U.K.
authors.forename: C H
authors.initials: CH
authors.lastname: Davies
authors.forename: M F
authors.initials: MF
authors.lastname: Pozza
authors.forename: G L
authors.initials: GL
authors.lastname: Collingridge
mesh_terms: D000818:Animals; D001418:Baclofen / Q000037:antagonists & inhibitors / Q000494:pharmacology; D005071:Evoked Potentials / Q000187:drug effects; D058788:GABA-B Receptor Antagonists; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D010721:Phosphinic Acids / Q000494:pharmacology*; D011412:Propanolamines / Q000494:pharmacology*; D051381:Rats; D018080:Receptors, GABA-B; D013569:Synapses / Q000187:drug effects / Q000378:metabolism; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
chemical_list: D058788:GABA-B Receptor Antagonists; D010721:Phosphinic Acids; D011412:Propanolamines; D018080:Receptors, GABA-B; C085075:CGP 55845A; D005680:gamma-Aminobutyric Acid; D001418:Baclofen