Note to users. If you're seeing this message, it means that your browser cannot find this page's style/presentation instructions -- or possibly that you are using a browser that does not support current Web standards. Find out more about why this message is appearing, and what you can do to make your experience of our site the best it can be.

Science 29 October 1982:
Vol. 218. no. 4571, pp. 487 - 490
DOI: 10.1126/science.7123250
Prev | Table of Contents | Next

Articles

Science, Vol 218, Issue 4571, 487-490
Copyright © 1982 by American Association for the Advancement of Science

articles

(+)-Amphetamine binding to rat hypothalamus: relation to anorexic potency for phenylethylamines

SM Paul, B Hulihan-Giblin, and P Skolnick

Saturable and stereospecific binding sites for (+)-[3H]amphetamine were demonstrated in membrane preparations from rat brain. The density of these binding sites varies among brain regions and is highest in the hypothalamus and brainstem. Specific (+)-[3H]amphetamine binding in hypothalamus is largely confined to synaptosomal membranes, rapidly reversible, and sensitive to both heat and proteolytic enzymes. Scatchard analysis of the equilibrium binding data revealed two distinct sites with apparent affinity constants of 93 and 300 nanomoles per liter, respectively. The effects of various psychotropic drugs as well as a number of putative neurotransmitters and related agonists and antagonists in displacing specific (+)-[3H]amphetamine binding demonstrate that these binding sites are not associated with any previously described neurotransmitter or drug receptors, but are specific for amphetamine and related phenylethylamine derivatives. Furthermore, the relative affinities of a series of phenylethylamine derivatives for (+)-[3H]amphetamine binding sites in hypothalamic membranes is highly correlated to their potencies as anorexic agents. These results suggest the presence of specific receptor sites in hypothalamus that mediate the anorexic activity of amphetamine and related drugs.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
Amphetamine Inhibits the N-Methyl-D-Aspartate Receptor-Mediated Responses by Directly Interacting with The Receptor/Channel Complex.
G.-C. Yeh, J.-C. Chen, H.-C. Tsai, H.-H. Wu, C.-Y. Lin, P.-C. Hsu, and Y.-C. Peng (2002)
J. Pharmacol. Exp. Ther. 300, 1008-1016
   Abstract »    Full Text »    PDF »
Current and Potential Drugs for Treatment of Obesity.
G. A. Bray and F. L. Greenway (1999)
Endocr. Rev. 20, 805-875
   Abstract »    Full Text »
Appetite Disturbance and Excessive Guilt in Major Depression: Use of Family Study Data to Define Depressive Subtypes.
J. F. Leckman, K. A. Caruso, B. A. Prusoff, M. M. Weissman, K. R. Merikangas, and D. L. Pauls (1984)
Arch Gen Psychiatry 41, 839-844
   Abstract »    PDF »
Analyzing nonlinear scatchard plots.
K. Light (1984)
Science 223, 76-78
   PDF »


To Advertise     Find Products

Science. ISSN 0036-8075 (print), 1095-9203 (online)