The picrotoxin-like action of a convulsant benzodiazepine, Ro5-3663

The picrotoxin-like action of a convulsant benzodiazepine, Ro5-3663

The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA 2 value of 3.97 to be calculated. Combination studies using the ‘classical’ GABA antagonists bicuculline and picroto...

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Veröffentlicht in:European journal of pharmacology 1983-01, Vol.87 (1), p.155-158
Hauptverfasser: Harrison, Neil L., Simmonds, Michael A.
Format: Artikel
Sprache:eng
Schlagworte:
1,3-dihydro-5-methyl 2H-1,4-benzodiazepine-2-one
Animals
Benzodiazepine
Benzodiazepinones - pharmacology
Bicuculline - pharmacology
Convulsant
Convulsants - pharmacology
GABA receptor
gamma -aminobutyric acid
In Vitro Techniques
medulla oblongata
Medulla Oblongata - metabolism
Muscimol - pharmacology
Neurons - metabolism
Picrotoxin
Picrotoxin - pharmacology
Rats
Receptors, Cell Surface - metabolism
Receptors, GABA-A
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Zusammenfassung:The potency and site of action of Ro5-3663 as a GABA antagonist were investigated in the rat cuneate slice in vitro. A Schild plot for Ro5-3663 was clearly non-linear but enabled a pA 2 value of 3.97 to be calculated. Combination studies using the ‘classical’ GABA antagonists bicuculline and picrotoxin indicated that Ro5-3663 acted at a separate site from bicuculline, but may share a common site with picrotoxin.
ISSN:0014-2999
1879-0712
DOI:10.1016/0014-2999(83)90064-X