PMID: 3760872Nov 1, 1986Paper

Characterization of high-affinity dopamine D2 receptors and modulation of affinity states by guanine nucleotides in cholate-solubilized bovine striatal preparations

Journal of Neurochemistry
S M KazmiRam K Mishra

Abstract

3,4-Dihydroxyphenylethylamine (dopamine) D2 receptors, solubilized from bovine striatal membranes using a cholic acid-NaCl combination, exhibited the typical pharmacological characteristics of both agonist and antagonist binding. The rank order potency of the agonists and antagonists to displace [3H]spiroperidol binding was the same as that observed with membrane-bound receptors. Computer-assisted analysis of the [3H]spiroperidol/agonist competition curves revealed the retention of high- and low-affinity states of the D2 receptor in the solubilized preparations and the proportions of receptor subpopulations in the two affinity states were similar to those reported in membrane. Guanine nucleotide almost completely converted the high-affinity sites to low-affinity sites for the agonists. The binding of the high-affinity agonist [3H]N-n-propylnorapomorphine ([3H]NPA) was clearly demonstrated in the solubilized preparations for the first time. Addition of guanylyl-imidodiphosphate completely abolished the [3H]NPA binding. When the solubilized receptors were subjected to diethylaminoethyl-Sephacel chromatography, the dopaminergic binding sites eluted in two distinct peaks, showing six- to sevenfold purification of the receptors in t...Continue Reading

References

May 1, 1985·The Journal of Pharmacy and Pharmacology·G J KilpatrickC D Marsden
Jan 1, 1984·Advances in Experimental Medicine and Biology·C TanakaN Kubo
Dec 15, 1984·Biochemical Pharmacology·W WoutersP M Laduron
Dec 1, 1983·Journal of Neurochemistry·J M HallP G Strange
Jan 1, 1983·Progress in Neuro-psychopharmacology & Biological Psychiatry·J Ramwani, R K Mishra
May 1, 1984·Journal of Neurochemistry·J Y Lew, M Goldstein
Apr 1, 1981·Proceedings of the National Academy of Sciences of the United States of America·S J List, P Seeman
Mar 26, 1982·European Journal of Pharmacology·B K MadrasP Seeman

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Citations

Nov 1, 1987·Molecular and Cellular Endocrinology·H B Niznik
Oct 21, 1998·The Journal of Steroid Biochemistry and Molecular Biology·S J EvansT F Murray
Apr 13, 2011·PLoS Neglected Tropical Diseases·Rita Bhardwaj, Patrick J Skelly
Jun 30, 1987·Biochimica Et Biophysica Acta·L K SrivastavaR K Mishra

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