The University of Southampton
University of Southampton Institutional Repository

Solubilization and characterization of ?-receptors from guinea pig brain membranes

Kavanaugh, M.P., Parker, Joel D., Bobker, D.H., Keana, J.F.W. and Weber, E. (1989) Solubilization and characterization of ?-receptors from guinea pig brain membranes Journal of Neurochemistry, 53, (5), pp. 1575-1580.

Record type: Article


The ?-receptor, a distinct binding site in brain tissue that may mediate some of the psychotomimetic properties of benzomorphan opiates and phencyclidine, has been sol-ubilized using the ionic detergent sodium cholate. Binding assays were performed with the solubilized receptor using vacuum filtration over polyethyleneimine-treated glass fiber filters. The pharmacological specificity of the solubilized binding site for ?-receptor ligands is nearly identical to the membrane-bound form of the receptor, with the order of potencies for displacement of the selective ?-ligand [3H]di-o-tolylguanidine ([3H]DTG) closely correlated. The stereoselectivity for (+)-benzomorphan opiate enantiomers was retained by the solubilized receptor. The soluble receptor retained high affinity for binding of [3H]DTG (KD= 28 ± 0.5 nM) and (+)-[3H]3-(3-hydroxyphenyl)-N-(l-propyl)piperi-dine {(+)-[3H]3-PPP} (KD= 36 ± 2 nM). Photoaffinity labeling of the solubilized receptor by [3H]p-azido-DTG, a ?-selective photoaffinity label, resulted in labeling of a 29-kilodalton polypeptide identical in size to that labeled in intact membranes. Estimation of the Stokes radius of the [3H]DTG binding site was obtained by Sepharose CL-6B chromatography in the presence of 20 mM cholate and calculated to be 8.7 nm. This value was identical to the molecular size found for the binding sites of the ?-selective ligands (+)-[3H]3-PPP and (+)-[3H]SKF-10,047, supporting the hypothesis that all three ligands bind to the same macro-molecular complex.

Full text not available from this repository.

More information

Published date: November 1989
Organisations: Biological Sciences


Local EPrints ID: 143689
ISSN: 0022-3042
PURE UUID: 06a721b6-4c5f-46e7-89be-48b06772dcbf

Catalogue record

Date deposited: 21 Jul 2010 10:47
Last modified: 27 Sep 2017 13:33

Export record


Author: M.P. Kavanaugh
Author: Joel D. Parker
Author: D.H. Bobker
Author: J.F.W. Keana
Author: E. Weber

University divisions

Download statistics

Downloads from ePrints over the past year. Other digital versions may also be available to download e.g. from the publisher's website.

View more statistics

Atom RSS 1.0 RSS 2.0

Contact ePrints Soton:

ePrints Soton supports OAI 2.0 with a base URL of

This repository has been built using EPrints software, developed at the University of Southampton, but available to everyone to use.

We use cookies to ensure that we give you the best experience on our website. If you continue without changing your settings, we will assume that you are happy to receive cookies on the University of Southampton website.