在大白鼠研究三甲基乙酸Buprenorphine酯具有長效止痛作用

Buprenorphine Pivalate Has A Long-acting Antinociceptive Effects in Rats

患有長時間疼痛的病患皆應希望能有一個具長效作用的止痛劑來解除疼痛。為了延長一個強效止痛劑Buprenorphine之藥效，我們合成了一個Buprenorphine醋即三甲基乙酸Buprenorphine醋，本研究的目的在評估這個酪是否具有長效作用。使用雄性SD大白鼠以縮腳掌反射來測試Buprenorphine及其背類之止痛作用，發現在大自鼠肌肉注射BuprenorphineHCl0.03,0.01及0.3µmol／kg可產生2、3及4小時之止痛作用。而肌肉注射三甲基乙酸Buprenorphine醋。.3,3及30µmol／kg可產生較長效的止痛作用，達48、52及54小時。在相同的給藥劑量下（0.3µmol／kg）•Buprenorphine HCl及三甲基乙酸Buprenorphine酪之止痛效期分別為4及48／J、時。我們作以下結論，在大鼠肌肉注射三甲基乙酸Buprenorphine酪可產生一個非常長的止痛作用，其效果為Buprenorphine HCl的12倍。

A long-acting analgesic is particularly desirable in patients with long-term pain. This study evaluates the antinociceptive effect and duration of action of a novel buprenorphine ester - buprenorphine pivalate - and shows whether this ester has a long-acting effect. The antinociceptive effects of buprenorphine HCl and pivalate were evaluated by using the plantar test in male Sprague-Dawley rats. We found that intramuscular injection of buprenorphine HCl 0.03, 0.1, and 0.3 µ mol/kg in rats produced dose-related antinociceptive effects of 2, 3, and 4 h, respectively. Intramuscular injection of buprenorphine pivalate 0.3, 3, and 30 µ mol/kg also produced dose-related antinociceptive effects, but with longer durations of action of 48, 52 and 54 h. Under an equi-molar basis of 0.3 µ mol/kg, the durations of action of intramuscular buprenorphine HCl and buprenorphine pivalate were 4 and 48 h, respectively. We conclude that intramuscular injection of buprenorphine pivalate produced a long-lasting antinociceptive effect which was much longer (12-fold) than intramuscular buprenorphine HCl.