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

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.

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Citation

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. (doi:10.1111/j.1471-4159.1989.tb08554.x).

More information

Published date: November 1989
Organisations: Biological Sciences

Identifiers

Local EPrints ID: 143689
URI: http://eprints.soton.ac.uk/id/eprint/143689
ISSN: 0022-3042
PURE UUID: 06a721b6-4c5f-46e7-89be-48b06772dcbf

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Date deposited: 21 Jul 2010 10:47
Last modified: 18 Jul 2017 23:09

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Contributors

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

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