Bianchetti A, Giudice A, Picerno N, Carminati P
Life Sci. 1982;31(20-21):2261-4. doi: 10.1016/0024-3205(82)90133-3.
A dissociation of the effects of the newly synthesized quaternary ammonium narcotic antagonist, levallorphan allyl bromide (CM 32191) on morphine-induced analgesia and constipation in the mouse is reported. CM 32191 behaved as a pure morphine antagonist on the "in vitro" preparation of longitudinal muscle of guinea-pig ileum and antagonized dose-dependently the peripherally mediated morphine constipation (ID50:15.6 mg/kg) without significantly affecting morphine analgesia (ID50: greater than 80 mg/kg). Its peripheral selectivity was greater than that of another quaternary ammonium compound, N-methyl naloxone. It is proposed as a useful pharmacological tool to differentiate the peripherally mediated from the centrally mediated effects of opioids.
据报道，新合成的季铵类麻醉拮抗剂烯丙基溴左洛啡烷（CM 32191）对小鼠吗啡诱导的镇痛和便秘作用存在解离现象。在豚鼠回肠纵肌的“体外”制备中，CM 32191表现为纯吗啡拮抗剂，能剂量依赖性地拮抗外周介导的吗啡便秘作用（半数抑制剂量：15.6毫克/千克），而对吗啡镇痛作用无明显影响（半数抑制剂量：大于80毫克/千克）。其外周选择性高于另一种季铵化合物N-甲基纳洛酮。它被认为是一种有用的药理学工具，可用于区分阿片类药物外周介导的作用和中枢介导的作用。
