Comparison Between the Interaction of Steroids with [35S]TBPS Binding to Cerebral Cortical and to Pituitary Membranes: Correlation with Inhibition of Prolactin Release

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 1992 Nov 1

PMID 1335125

Citations 1

Authors

M Vincens

C Shu

M Fortin

D Philibert

Affiliations

Soon will be listed here.

Abstract

It has been shown previously that 5 alpha-pregnan-3 alpha-ol-20-one (5 alpha 3 alpha P) can inhibit prolactin release from anterior pituitary gland cells in culture through an interaction with a specific modulatory site on the GABAA receptor complex in anterior pituitary gland membranes. In the present work, this receptor site has been labelled with [35S]t-butylbicyclophosphorothionate ([35S]TBPS) to enable a study of the relative binding affinities (RBA) of different steroids for the GABAA receptor complex to be made. We have found a high correlation (r = +0.88) between the inhibition of [35S]TBPS binding to anterior pituitary membranes and the inhibition of [35S]TBPS binding to cerebral cortical membranes by nine different steroids. There was also a high correlation between the inhibition of prolactin release from anterior pituitary gland cells in culture by these steroids and the inhibition of [35S]TBPS binding to anterior pituitary membranes (r = +0.99) or to cortical membranes (r = +0.81). These observations suggest that the measurement of prolactin release from anterior pituitary gland cells in culture is a good indicator of the functional activity of drugs that bind to the allosteric modulatory TBPS-binding site on the GABAA-receptor complex.

Citing Articles

An autoradiographic study comparing the interactions of 3 alpha-OH-5 alpha-pregnan-20-one, pregnenolone sulfate and pentobarbital with [3S]-TBPS binding sites and their modulation by GABA in different structures of the rat brain.

Vincens M, Dartois E, Moyse E, Haour F, Fillion G Naunyn Schmiedebergs Arch Pharmacol. 1995; 351(4):356-62.

PMID: 7630426 DOI: 10.1007/BF00169075.

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