The peripheral-type benzodiazepine receptor is present in astrocytes but is not a primary site of action for convulsants/anticonvulsants.

Abstract:

:High-affinity binding sites for [3H]PK 11195 and [3H]Ro 5-4864 with the properties of the peripheral-type benzodiazepine receptor were detected in primary cultures of both mouse neocortical and cerebellar astrocytes. The binding sites were enriched in mitochondrial fractions on differential centrifugation. An 18-kDa polypeptide was specifically photolabelled in cerebellar astrocytes by [3H]PK 14105, a photolabel for the peripheral-type benzodiazepine receptor. However, this polypeptide did not show any reactivity with an antiserum previously raised against the corresponding polypeptide from rat adrenal gland. Various anticonvulsant and convulsant agents were tested for their ability and potency at inhibiting [3H]Ro 5-4864 binding to neocortical astrocytes. Many of these compounds previously reported to be inhibitors of diazepam binding to neocortical astrocytes, proved ineffective in this study. No correlation was observed between convulsant/anticonvulsant potency and ability to inhibit [3H]Ro 5-4864 binding to the peripheral-type benzodiazepine receptor in these cells. Thus, whereas some convulsants and anticonvulsants might interact with this astrocytic receptor, such a system has no validity as a general screening method for these agents.

journal_name

J Neurochem

authors

Moynagh PN,Schousboe A,Williams DC

doi

10.1046/j.1471-4159.1994.62020673.x

subject

Has Abstract

pub_date

1994-02-01 00:00:00

pages

673-9

issue

2

eissn

0022-3042

issn

1471-4159

journal_volume

62

pub_type

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