Competitive interactions at [3H]1,3-di(2-tolyl)guanidine (DTG)-defined sigma recognition sites in guinea pig brain.

Abstract:

:In saturation binding experiments, (+)pentazocine, (+)3-(3-hydroxyphenyl)-N-propylpiperidine (3-PPP), haloperidol and rimcazole did not inhibit the binding of [3H]DTG in a purely competitive fashion. Although Scatchard analysis indicated that [3H]DTG bound to a single site, the inhibition curves of some, but not all, reference compounds exhibited Hill coefficients of less than 0.8. The Scatchard data were consistent with a model of hyperbolic competitive inhibition of binding to the [3H]DTG-defined sigma site, although other possibilities such as negative cooperativity or binding to two sites cannot be definitively excluded. Compounds from numerous pharmacological and structural classes inhibited the binding of [3H]DTG, suggesting that interactions of [3H]DTG with other receptors may have confounded the Scatchard analysis of the binding of [3H]DTG to sigma recognition sites.

journal_name

Life Sci

journal_title

Life sciences

authors

DeHaven-Hudkins DL,Fleissner LC

doi

10.1016/0024-3205(92)90255-n

subject

Has Abstract

pub_date

1992-01-01 00:00:00

pages

PL65-70

issue

9

eissn

0024-3205

issn

1879-0631

pii

0024-3205(92)90255-N

journal_volume

50

pub_type

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