Synthetic Analgesics: Stereochemical Considerations

Abstract

Summary The evidence is presented for the probability of the activity exhibited by analgesics and their antagonists being due to their association with a specific receptor surface. The configurations of those isomers exhibiting nearly all the activity of certain racemic mixtures are identical, and related to that of D-(–)-alanine; the stereochemical requirements of analgesics are considered. Active analgesics are shown to have structures which enable them to present similar surfaces to allow of their association with a proposed “analgesic receptor surface,” the essential features of which are described. A number of essential structures are outlined as prerequisites for compounds designed as analgesics.