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Interaction of Dihydroxy-2-Aminotetralin Derivatives at Sites Labelled With [<sup>3</sup>H]Clonidine, [<sup>3</sup>H]Prazosin and [<sup>3</sup>H]Spiperone in Rat Brain MembranesChatterjee, Tapan K., Bhatnagar, Ranbir K., Cannon, Joseph G., Long, John P. 17 February 1984 (has links)
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.
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