Hiyama T, Shintani S, Tsutsui M, Yasuda Y
Nihon Yakurigaku Zasshi. 1982 Mar;79(3):147-62.
Pharmacological properties of buprenorphine were studied in comparison with those of morphine and pentazocine. Buprenorphine was more potent than morphine and pentazocine in analgesic tests, using chemical, thermal, pressure, and electrical stimulation as the nociceptive stimuli. Buprenorphine exhibited analgesic activity in the D' Amour-Smith's test at high stimulus intensity and in the Haffner's test, while pentazocine exhibited little or no analgesic action in these tests. Buprenorphine showed a bell-shaped dose-response curve in the mouse D'Amour-Smith's test at high stimulus intensity. Analgesic action of buprenorphine was antagonized by naloxone administered before buprenorphine, but not antagonized by naloxone administered after buprenorphine. Duration of the analgesic action of buprenorphine was longer than those of morphine and pentazocine. Buprenorphine decreased the amplitudes of evoked potentials which were recorded from the nucleus ventralis posteromedialis, nucleus centralis lateralis, and periaquaductal central gray. As a naloxone antagonist, Buprenorphine was equivalent or less potent than naloxone and more potent than pentazocine. Tolerance developed to the analgesic activity of buprenorphine, but development of tolerance to buprenorphine was less than that of tolerance to morphine. It was concluded that buprenorphine may be a useful analgesic drug because of its high intrinsic activity and long duration of action.
对丁丙诺啡的药理特性进行了研究,并与吗啡和喷他佐辛进行了比较。在以化学、热、压力和电刺激作为伤害性刺激的镇痛试验中,丁丙诺啡比吗啡和喷他佐辛更有效。在高刺激强度的D’阿莫尔-史密斯试验和哈夫纳试验中,丁丙诺啡表现出镇痛活性,而喷他佐辛在这些试验中几乎没有或没有镇痛作用。在高刺激强度的小鼠D’阿莫尔-史密斯试验中,丁丙诺啡呈现钟形剂量反应曲线。丁丙诺啡给药前给予纳洛酮可拮抗其镇痛作用,但丁丙诺啡给药后给予纳洛酮则不能拮抗。丁丙诺啡的镇痛作用持续时间比吗啡和喷他佐辛更长。丁丙诺啡降低了从腹后内侧核、外侧中央核和导水管周围中央灰质记录的诱发电位幅度。作为一种纳洛酮拮抗剂,丁丙诺啡的效力与纳洛酮相当或低于纳洛酮,高于喷他佐辛。丁丙诺啡的镇痛活性会产生耐受性,但对丁丙诺啡耐受性的产生低于对吗啡耐受性的产生。得出的结论是,由于丁丙诺啡具有高内在活性和长作用持续时间,它可能是一种有用的镇痛药。