D. Rusterholz, S. Dryer, J. P. Long
Jul 25, 1980
Citations
0
Influential Citations
17
Citations
Quality indicators
Journal
European Journal of Pharmacology
Abstract
Abstract Three 5,8-dimethoxylated derivatives of 2-aminotetralin (2-AT) were compared with clonidine, methoxamine and phenylephrine in tests for sedation (inhibition of exploratory activity) and analgesia. In both tests the 2-AT derivatives were less potent than clonidine, but more potent than methoxamine or phenylephrine. Antagonism of the 2-AT derivative, DR-31, and clonidine by yohimbine in both tests argues for the involvement of α 2 -adrenoreceptors in the mediation of these behavioral effects. α 1 -Adrenoreceptors also mediate an inhibition of exploratory activity since the inhibition induced by methoxamine was antagonized by phenoxybenzamine (POB) but not by yohimbine. The methoxylated 2-AT derivatives, which have previously been shown to exert potent peripheral α 1 -agonism are now demonstrated to have sedative and anlgesic effectscharacteristic of central α 2 -adrenergic stimulation.