Abstract
Pharmacologic studies on a new analgesic agent, azabicyclane (4β-methoxy-1-methyl-4α-phenyl-3α,5α-propanopiperidine hydrogen citrate) were carried out and compared with meperidine HCl. Azabicyclane showed an analgesic potency about 3 times greater than meperidine by mechanical, chemical, and thermal stimulation methods in mice and rats. Adverse side effects, such as mydriasis, hypotension, and local irritation, were less pronounced with azabicyclane than with meperidine at equianalgesic doses. Similar antagonism to analgesic effect by nalorphine, rapid development of tolerance to analgesic effect, antitussive effect, potentiation of thiopental anesthesia, and slight respiratory depression were observed with both drugs. Clear physical dependence liability was not demonstrated in rats by azabicyclane or meperidine. The acute toxicity of azabicyclane was almost the same as that of meperidine.
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