Acteo M D, Bowman E, Butelman E, Englis J A, Harrish L, Jacobson A E, Mattson M V, Medzihradsky F, Patrick G, Rowlett J K, Smith C B, Winger G, Woods J H, Woolverton W L
Department of Pharmacology, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0163, USA.
Drug Alcohol Depend. 1996 Oct;42(2):93-104. doi: 10.1016/0376-8716(96)01267-7.
Zipeprol was evaluated in a number of in vitro and in vivo assays predictive of stimulant, depressant, or opioid abuse potential. Zipeprol had affinity for mu and kappa opioid binding sites as well as sigma binding sites. However, it failed to exert opioid-like agonist actions in rodents, and did not attenuate withdrawal signs in morphine- or pentobarbital-dependent rats. Zipeprol did not substitute for either amphetamine or pentobarbital in drug discrimination assays in rhesus monkeys. On the other hand, it suppressed morphine withdrawal signs in rhesus monkeys in two assays, and it acted as a quadazocine-sensitive reinforcer in monkeys trained to self-inject alfentanil. Zipeprol also acted as a reinforcer in monkeys trained to self-inject methohexital. In a dose range of 10-18 mg/kg, zipeprol induced convulsions in monkeys. Zipeprol appears to have abuse potential and a novel spectrum of action involving both opioid and non-opioid effects.
在一系列预测兴奋剂、抑制剂或阿片类药物滥用可能性的体外和体内试验中对齐培丙醇进行了评估。齐培丙醇对μ和κ阿片受体结合位点以及σ结合位点具有亲和力。然而，它在啮齿动物中未能发挥类阿片激动剂作用，并且在吗啡或戊巴比妥依赖的大鼠中也未减轻戒断症状。在恒河猴的药物辨别试验中，齐培丙醇不能替代苯丙胺或戊巴比妥。另一方面，在两项试验中它抑制了恒河猴的吗啡戒断症状，并且在训练有素的自我注射阿芬太尼的猴子中它作为一种对喹唑嗪敏感的强化剂起作用。齐培丙醇在训练有素的自我注射甲己炔巴比妥的猴子中也作为一种强化剂起作用。在10 - 18毫克/千克的剂量范围内，齐培丙醇在猴子中诱发惊厥。齐培丙醇似乎具有滥用可能性以及涉及阿片类和非阿片类效应的新型作用谱。
