Interaction of dihydroxy-2-aminotetralin derivatives at sites labelled with [3H]clonidine, [3H]prazosin and [3H]spiperone in rat brain membranes.
The interactions of 5,6- and 6,7-dihydroxy derivatives of 2-aminotetralin with [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]peiperone binding sites while for [3H]prazosin binding site these agents appeared virtually inactive. For interaction with [3H]clonidine binding site 6,7-dihyroxy substitutions impart greater potency that 5,6-dihydroxy substitutions and N-alkyl substitutions either make no differece or reduce the affinity of these compounds. N-alkyl substitutions, however, markedly enhance the affinity of 5,6-dihydroxy derivatives for interaction with [3H]spiperone binding site. The results suggest that some hydroxy derivatives of aminotetralin have significant interaction with both central alpha 2-adrenoceptor and D2-dopamine receptor systems.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000378:metabolism* / Q000648:ultrastructure; D002090:Butyrophenones / Q000494:pharmacology*; D002462:Cell Membrane / Q000378:metabolism; D002540:Cerebral Cortex / Q000378:metabolism; D003000:Clonidine / Q000494:pharmacology*; D004347:Drug Interactions; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D011224:Prazosin / Q000494:pharmacology*; D011799:Quinazolines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013134:Spiperone / Q000494:pharmacology*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*
D002090:Butyrophenones; D009281:Naphthalenes; D011799:Quinazolines; D013764:Tetrahydronaphthalenes; C006561:2-aminotetralin; D013134:Spiperone; D003000:Clonidine; D011224:Prazosin