Heilman R D, Gray M I, Chen R P, Hahn E F, Fishman J
Res Commun Chem Pathol Pharmacol. 1976 Apr;13(4):635-47.
The mouse hot plate model, with slight differences from the way it is used to study narcotic analgesics, was evaluated as a method for determining the oral effectiveness, relative potency and duration of action of two standard narcotic antagonists, naloxone and naltrexone, and a new agent, 6-desoxy-6-methylene-naltrexone (ORF 11676). Naltrexone and ORF 11676 were found to be more effective orally than naloxone. Naltrexone and ORF 11676 were equipotent by 3 routes of administration and both were more potent than naloxone. Naloxone produced a significantly shorter duration of action than the other two drugs. It was concluded that the mouse hot plate method, used to detect and characterize the activity of narcotic antagonists, provides information compatible with that obtained in other species, including man.
小鼠热板模型与用于研究麻醉性镇痛药的方式略有不同,该模型被评估为一种用于确定两种标准麻醉性拮抗剂纳洛酮和纳曲酮以及一种新药6-去氧-6-亚甲基-纳曲酮(ORF 11676)的口服有效性、相对效价和作用持续时间的方法。结果发现,纳曲酮和ORF 11676口服比纳洛酮更有效。纳曲酮和ORF 11676通过三种给药途径等效,且两者都比纳洛酮更有效。纳洛酮的作用持续时间明显短于其他两种药物。得出的结论是,用于检测和表征麻醉性拮抗剂活性的小鼠热板法所提供的信息与在包括人类在内的其他物种中获得的信息一致。