Synthesis and Analgesic Activity of Some Condensed Analogs of Anpirtoline

Abstract

New condensed derivatives of anpirtoline, in which the pyridine ring is replaced with quinoline, isoquinoline, quinazoline, and phthalazine nuclei, have been synthesized. Their receptor binding profiles (5‐HT1A, 5‐HT1B) and analgesic activity (hot plate, acetic acid induced writhing) have been studied. The analgesic activity of compounds 7d, 8b, 8c, and 8e are at least comparable to that of the clinically used drugs flupirtine and tramadol under the same conditions.

Synthesis, Analgesic Activity, and Binding Properties of Some Epibatidine Analogs with a Tropine Skeleton

“…On the other hand, the analgesic activity of anpirtoline is supposed to be mediated by 5-HT 1B receptors and involvement of 5-HT 1A receptors in analgesic activity of some active compounds is also anticipated [22,23] . Recently also analgesic activity of several types of anpirtoline analogs has been reported [27][28][29][30] . Many muscarinic cholinergic agonists have been studied as potential antinociceptive agents.…”