阿片类药物和阿片类拮抗剂对小鼠斯特劳布尾反应的影响。

Effects of opiates and opiate antagonists on the Straub tail reaction in mice.

Aceto M D, McKean D B, Pearl J

Br J Pharmacol. 1969 Jun;36(2):225-39. doi: 10.1111/j.1476-5381.1969.tb09500.x.

Abstract

Subcutaneous injections of opiates produced the Straub tail reaction in mice. The potencies of the opiates in mice were consistent with previous estimates of the analgesic potencies in animals and in man.2. The potencies of sixteen antagonists in counteracting the reaction were consistent with those previously obtained with the rat tail-flick test.3. The (-) isomers of four benzomorphan derivatives were much more potent in counteracting the reaction than their (+) isomers and about twice as potent as their racemates. The activity of the isomers seemed to follow Pfeiffer's rule: the lower the effective dose of a drug, the greater the difference in the pharmacological effects of the optical isomers. One of the trans isomers acted like an opiate, while its cis isomer acted like an antagonist.4. Naloxone and nalorphine fulfilled conventional criteria for competitive antagonism, whereas atropine and the (-) and the (+) isomers of pentazocine and of cyclazocine did not do so.5. The Straub tail test seems to be useful for studying structure-activity relations among opiates and opiate antagonists.

摘要

皮下注射阿片类药物可使小鼠产生斯特劳布尾反应。阿片类药物在小鼠体内的效价与先前对动物和人类镇痛效价的估计一致。
十六种拮抗剂对抗该反应的效价与先前通过大鼠甩尾试验得到的结果一致。
四种苯并吗啡烷衍生物的（-）异构体在对抗该反应方面比其（+）异构体效力强得多，且效力约为其外消旋体的两倍。异构体的活性似乎遵循普费弗法则：药物的有效剂量越低，光学异构体药理作用的差异就越大。其中一种反式异构体的作用类似于阿片类药物，而其顺式异构体的作用则类似于拮抗剂。
纳洛酮和纳洛芬符合竞争性拮抗的传统标准，而阿托品以及喷他佐辛和环佐辛的（-）和（+）异构体则不符合。
斯特劳布尾试验似乎有助于研究阿片类药物和阿片类拮抗剂之间的构效关系。