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CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 2001 Mar; Vol. 415 (2-3), pp. 191-5. - Publication Year :
- 2001
-
Abstract
- In rat neocortical preparations maintained in Mg(2+)-free Krebs medium, baclofen depressed the frequency of spontaneous discharges in a concentration-dependent manner (EC(50) = 6 microM), sensitive to (3-aminopropyl)ethylphosphinic acid (CGP 36216) (100, 300 and 500 microM) (pA(2) = 3.9 +/- 0.1). By contrast, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid(B) (GABA(B)) postsynaptic receptors. In electrically stimulated brain slices preloaded with [3H]GABA, CGP 36216 increased [3H]GABA release (IC(50) = 43 microM), which was reversed by baclofen (20 microM). While CGP 36216 is ineffective at GABA(B) postsynaptic receptors, it is appreciably more active at presynaptic receptors.
- Subjects :
- Animals
Autoreceptors metabolism
Baclofen pharmacology
Dose-Response Relationship, Drug
GABA Agonists pharmacology
Male
Neocortex metabolism
Organophosphorus Compounds chemistry
Organophosphorus Compounds pharmacology
Phosphinic Acids pharmacology
Rats
Rats, Sprague-Dawley
Receptors, GABA-B metabolism
gamma-Aminobutyric Acid metabolism
Autoreceptors drug effects
GABA Antagonists pharmacology
Neocortex drug effects
Receptors, GABA-B drug effects
gamma-Aminobutyric Acid drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 415
- Issue :
- 2-3
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 11274998
- Full Text :
- https://doi.org/10.1016/s0014-2999(01)00842-1