Yamamoto H, Saito C, Inaba S, Inukai T, Kobayashi K
Arzneimittelforschung. 1975 May;25(5):795-801. doi: 10.1002/chin.197534266.
A new non-narcotic analgesic, 2-[3-(p-fluorobenzoyl)-n-propy]-5alpha,9alpha-dimethyl-2'-hydroxy-6,7-benzomorphan (ID-1229) has been prepared from 5alpha,9alpha-dimethyl-2'-hydroxy-6,7-benzomorphan. The analgesic activities of ID-1229 were several times more potent than those of pentazocine in the acetic acid writhing test in mice, bradykinin test in rats, Randall-Selitto's test in rats, and the electrical stimulation test in mice, while, ID-1229 showed little activity in both the tail pinch test and the hot plate test. ID-1229 did not show anti-narcotic activity in the morphine-combined test, and the Straub tail phenomenon was not observed in ID-1229. ID-1229 showed CNS activities in some tranquilizing tests, but did not show activity in several other CNS tests. The CNS potency is condiserably weaker as compared with haloperidol or diazepam, and the pattern of CNS activities in ID-1229 is quite different from those of both compounds. ID-1229 is a potent non-narcotic analgesic with tranquilizing activity, which is quite free from the undersirable side effects of morphine or morphine-like compounds including pentazocine.
一种新的非麻醉性镇痛药，2-[3-(对氟苯甲酰基)-正丙基]-5α,9α-二甲基-2'-羟基-6,7-苯并吗啡烷（ID-1229）已由5α,9α-二甲基-2'-羟基-6,7-苯并吗啡烷制备而成。在小鼠醋酸扭体试验、大鼠缓激肽试验、大鼠Randall-Selitto试验以及小鼠电刺激试验中，ID-1229的镇痛活性比喷他佐辛强数倍，而在夹尾试验和热板试验中，ID-1229几乎没有活性。在吗啡联合试验中，ID-1229未表现出抗麻醉活性，且未观察到ID-1229的Straub尾现象。ID-1229在一些安定试验中表现出中枢神经系统活性，但在其他一些中枢神经系统试验中未表现出活性。与氟哌啶醇或地西泮相比，其对中枢神经系统的作用强度明显较弱，且ID-1229的中枢神经系统活性模式与这两种化合物均有很大不同。ID-1229是一种具有安定活性的强效非麻醉性镇痛药，完全没有吗啡或包括喷他佐辛在内的吗啡样化合物的不良副作用。
