Interaction of Dihydroxy-2-Aminotetralin Derivatives at Sites Labelled With [3H]Clonidine, [3H]Prazosin and [3H]Spiperone in Rat Brain Membranes
Document Type
Article
Publication Date
2-17-1984
Description
The interactions of 5,6- and 6,7-dihydroxy derivatives of 2-aminotetralin with [3H]clonidine and [3H]clonidine and [3H]prazosin as well as with [3H]spiperone binding sites in rat cerebral cortex membrane preparations were investigated. The hydroxy derivatives of 2-aminotetralin tested showed significant interaction with [3H]clonidine as well as with [3H]spiperone binding sites while for [3H]prazosin binding site these agents appeared virtually inactive. For interaction with [3H]clonidine binding site 6,7-dihydroxy substitutions impart greater potency that 5,6-dihydroxy substitutions and N-alkyl substitutions either make no difference or reduce the affinity of these compounds. N-alkyl substitutions, however, markedly enhance the affinity of 5,6-dihydroxy derivatives for interactions with [3H]spiperone binding site. The results suggest that some hydroxy derivatives of aminotetralin have significant interaction with both central α2-adrenoceptor and D2-dopamine receptor systems.
Citation Information
Chatterjee, Tapan K.; Bhatnagar, Ranbir K.; Cannon, Joseph G.; and Long, John P.. 1984. Interaction of Dihydroxy-2-Aminotetralin Derivatives at Sites Labelled With [3H]Clonidine, [3H]Prazosin and [3H]Spiperone in Rat Brain Membranes. European Journal of Pharmacology. Vol.98(2). 293-296. https://doi.org/10.1016/0014-2999(84)90605-8 PMID: 6714312 ISSN: 0014-2999