Pharmacological Features Of Several Novel Irreversible Opioid Agonists And Molecular Reactions Between Them And Opioid Receptors

During the study on novel ultralong-lasting narcotic analgesics, we found out several irreversible opioid agonists, α-CAM and FI-11 and its analgus. we studied their pharmacological effects both in vivo and in vitro, and investigated the mocecular reactions between opioid receptors and the novel irreversible agonists, α-CAM and FI-11.Our results show that α-CAM, a derivative of oripavine, is a novel universal irreversible opioid agonists. In the receptor binding assay, α-CAM could irreversiblly inhibited. the binding of [⁸H] Etorphine (Etor) with P₂ membrane of rat brain; In isolated tissue bioassays, it inhibited, in a wash-resistant manner, the...