In vitro and in vivo characterisation of buprenorphine and other long-lasting opioids

Buprenorphine is a promising medication for the treatment of opiate abuse. The pharmacology of buprenorphine has been studied in vitro using radioligand binding and [-35S]GTPyS assays, and in vivo using assays of antinociception in rodents. A number of compounds with potential similar pharmacology have also been characterised. These are an iso-morphinan pyrrolidine derivative, and long-lasting 14-aminomorphinones and codeinones, in particular clocinnamox (C-CAM), a pure μ-antagonist and methoclocinnamox (MC-CAM), which has some agonist properties.... cont'd.