THIP and isoguvacine are partial agonists of GABA-stimulated benzodiazepine receptor binding.

Abstract:

:The effects of THIP and isoguvacine on 3H-flunitrazepam binding to washed membranes prepared from the cerebral cortex of adult rats have been examined. THIP, which has only minimal stimulatory effects on benzodiazepine (BZ) receptor binding, has been found to inhibit the stimulation induced by small concentrations (2 microM) of exogenous GABA. While isoguvacine stimulates BZ receptor binding, although to a smaller extent than GABA, it also antagonizes the stimulation of BZ receptor binding induced by GABA. Thus THIP and isoguvacine exhibit the properties of a partial agonist of GABA-stimulated BZ receptor binding.

journal_name

Eur J Pharmacol

authors

Karobath M,Lippitsch M

doi

10.1016/0014-2999(79)90321-2

subject

Has Abstract

pub_date

1979-10-15 00:00:00

pages

485-8

issue

4

eissn

0014-2999

issn

1879-0712

pii

0014-2999(79)90321-2

journal_volume

58

pub_type

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