AGONIST AND ANTAGONIST PROPERTIES OF BUPRENORPHINE, A NEW ANTINOCICEPTIVE AGENT

摘要: 1. Buprenorphine is a highly lipophilic derivative of oripavine. In rodent antinociceptive assays (writhing, tail pressure), buprenorphine had an action which was rapid in onset and long duration; it 25-40 times more potent than morphine after parenteral injection 7-10 oral administration. 2. The log dose-response relationship for curvilinear mouse rat flick tests with the effect decreasing at higher, non-toxic doses. 3. Tolerance developed to activity mice. 4. No signs abstinence were observed on naloxone challenge or abrupt withdrawal monkeys receiving chronically one month. 5. antagonized actions but ineffective antagonist pressure test. 6. precipitated morphine-dependent mice not rats. 7. produced Straub tails This when animals pretreated naloxone. However, test high doses diprenorphine established effects buprenorphine. 8. It concluded that represents definite advance search narcotic analgesic low physical dependence potential.