Discrimination of (+)-3-PPP sites from DTG sites by FH-510, a novel potent sigma ligand, in rat brain.

Abstract:

:The effect of 5,8-dimethyl-4-(2-di-n-propylaminoethyl)carbazol monohydrochloride (FH-510) on the binding of sigma ligands such as [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H](+)-3-PPP) and [3H]1,3-di-o-tolylguanidine ([3H]DTG) to rat brain membranes was studied. The inhibitory effect of FH-510 on [3H](+)-3-PPP binding to membranes of rat brain was 260 times more potent than that on [3H]DTG binding. Scatchard plot analysis showed that FH-510 inhibited [3H](+)-3-PPP binding in a competitive manner, while the inhibitory effect of FH-510 on [3H]DTG binding was noncompetitive. These results suggest that (+)-3-PPP sites could be discriminated from DTG sites, and that FH-510 binds preferentially to (+)-3-PPP recognition sites in rat brain.

journal_name

Eur J Pharmacol

authors

Chaki S,Tanaka M,Muramatsu M,Otomo S

doi

10.1016/0014-2999(93)90638-x

subject

Has Abstract

pub_date

1993-11-30 00:00:00

pages

173-5

issue

1

eissn

0014-2999

issn

1879-0712

pii

0014-2999(93)90638-X

journal_volume

250

pub_type

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