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R-(-)-beta-phenyl-GABA is a full agonist at GABAB receptors in brain slices but a partial agonist in the ileum.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1993 Mar 16; Vol. 233 (1), pp. 169-72. - Publication Year :
- 1993
-
Abstract
- R-(-)-beta-phenyl-GABA has been compared at GABAB receptors using cortical and ileal preparations. R-(-)-beta-phenyl-GABA (EC50 = 25 microM) was a less potent full agonist than R,S-(+/-)-baclofen (EC50 = 2.5 microM), in depressing CA1 population spikes of rat hippocampal slices, and 5 times less potent in attenuating the spontaneous discharges of rat neocortex. However, R-(-)-beta-phenyl-GABA (100-400 microM) was only a weak partial agonist in the ileum. All these actions were sensitive to CGP 35348 (3-aminopropyl-(P-diethoxymethyl)-phosphinic acid) and therefore mediated by GABAB receptors.
- Subjects :
- Animals
Cerebral Cortex drug effects
Cerebral Cortex metabolism
Guinea Pigs
Hippocampus drug effects
Hippocampus metabolism
Ileum drug effects
In Vitro Techniques
Male
Organophosphorus Compounds pharmacology
Rats
Rats, Sprague-Dawley
Stereoisomerism
gamma-Aminobutyric Acid pharmacology
Brain Chemistry drug effects
Muscle, Smooth drug effects
Receptors, GABA-A drug effects
Tranquilizing Agents pharmacology
gamma-Aminobutyric Acid analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 233
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 8386087
- Full Text :
- https://doi.org/10.1016/0014-2999(93)90364-n