Stockhaus K, Ensinger H A, Gaida W, Jennewein H M, Merz H
NIDA Res Monogr. 1983 Apr;43:144-9.
Mr 2033 CL is a very potent non-morphine-like opioid analgesic as shown in different test models and animal species. On a weight for weight basis, it is about 20 times more potent than morphine. The analgesic effects of Mr 2033 CL are supposed to be different from those of morphine and bremazocine because of individual sensitivity against selective antagonists like naloxone and Mr 2266 CL. Mr 2033 CL does not induce the Straub tail phenomenon and increased circling movements in mice, catatonia in rats, and stupor in rabbits which are characteristic for mu agonists. Moreover, Mr 2033 CL does not have a morphine-like abuse potential in rats, dogs and rhesus monkeys. CNS-depressive effects were observed in different species. Respiratory depression and inhibition of intestinal transit seem to be of minor degree. In contrast to morphine, Mr 2033 CL provokes diuresis in rats. Binding studies in rats as well as dependence studies in rats and rhesus monkeys characterize Mr 2033 CL as a predominant kappa agonist with morphine antagonistic properties.
在不同的测试模型和动物物种中，Mr 2033 CL是一种非常强效的非吗啡类阿片类镇痛药。按重量计算，其效力约为吗啡的20倍。由于对纳洛酮和Mr 2266 CL等选择性拮抗剂的个体敏感性，Mr 2033 CL的镇痛作用被认为与吗啡和布马佐辛不同。Mr 2033 CL不会诱发小鼠的Straub尾现象和增加转圈运动、大鼠的紧张症以及兔子的昏迷，这些是μ激动剂的特征。此外，Mr 2033 CL在大鼠、狗和恒河猴中没有吗啡样的滥用潜力。在不同物种中观察到了中枢神经系统抑制作用。呼吸抑制和肠道运输抑制似乎程度较轻。与吗啡不同，Mr 2033 CL可引起大鼠利尿。大鼠的结合研究以及大鼠和恒河猴的依赖性研究表明，Mr 2033 CL是一种主要的κ激动剂，具有吗啡拮抗特性。
