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The effect of GABA on in vitro binding of two novel non-benzodiazepines, PK 8165 and CGS 8216, to benzodiazepine receptors in the rat brain.

Abstract：

:The effect of gamma-aminobutyric acid (GABA) on the binding of PK 8165, a quinoline derivative, and CGS 8216, a pyrazoloquinoline, was assessed in two different regions of the rat brain. PK 8165, a compound with reported anxiolytic properties, inhibited [3H]-propyl beta-carboline-3-carboxylate labeled receptors in the cerebellum with an IC50 of 844 nM and 370 nM in the absence and presence of micro M GABA, respectively. GABA (100 micro M) was less effective in the cerebral cortex, decreasing the IC50 value from 280 to 197 nM. In saturation isotherm studies with [3H]-CGS 8216, a benzodiazepine receptor antagonist, GABA (100 micro M) induced a small but significant reduction in the apparent affinity of [3H]-CGS 8216 for benzodiazepine receptors in the cerebral cortex but the Bmax was unchanged.

journal_name

Life Sci

journal_title

Life sciences

authors

Morelli M,Gee KW,Yamamura HI

doi

10.1016/0024-3205(82)90403-9

subject

Has Abstract

pub_date

1982-07-05 00:00:00

pages

77-81

issue

1

eissn

0024-3205

issn

1879-0631

pii

0024-3205(82)90403-9

journal_volume

31

pub_type

杂志文章

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