Stereospecific interaction of bicuculline with specific [3H]strychnine binding to rat spinal cord synaptosomal membranes.

Abstract:

:The gamma-aminobutyric acid (GABA) antagonist (+/-)-bicuculline inhibits specific [3H]strychnine binding to postsynaptic glycine receptor sites in rat spinal cord synaptosomal membranes with an inhibition constant of about 5 microM, which is fairly similar to its inhibition constant reported for the GABA receptor. This effect is highly stereospecific, since the affinity of (-)-bicuculline for the specific [3H]strychnine binding sites is more than ten times less than that of the pharmacologically active (+)-bicuculline. Besides an unspecific effect at the glycine receptor, the results could suggest that the glycine and the GABA receptors are located close together in spinal cord membranes, so that the antagonist states of both receptors may be able to interfere with each other in some mechanistic way.

journal_name

Neurosci Lett

journal_title

Neuroscience letters

authors

Goldinger A,Müller WE

doi

10.1016/0304-3940(80)90107-x

subject

Has Abstract

pub_date

1980-01-01 00:00:00

pages

91-5

issue

1

eissn

0304-3940

issn

1872-7972

pii

0304-3940(80)90107-X

journal_volume

16

pub_type

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