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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.

Authors :
Ong J
Kerr DI
Doolette DJ
Duke RK
Mewett KN
Allen RD
Johnston GA
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.

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