Malec D, Langwiński R
Pol J Pharmacol Pharm. 1983;35(4):293-300.
We investigated the effect of benzhydramine, thenalidine, mepyramine (H1 receptor antagonists) and cimetidine (H2 receptor antagonist) on cataleptogenic action of morphine, codeine, fentanyl, and haloperidol. Benzhydramine antagonized the catalepsy induced by analgesics (particularly by codeine). The antagonistic effect of thenalidine was weaker (but also very prominent for codeine catalepsy). Mepyramine did not affect the catalepsy induced by analgesics. All three H1 receptor antagonists attenuated the catalepsy induced by haloperidol. Cimetidine, injected intraventricularly, did not affect the catalepsy induced either by analgesics or by haloperidol. It is suggested that the antagonistic action of benzhydramine and thenalidine against analgesic catalepsy is related rather to their antiserotonin properties, while the anticataleptic activity of all three H1 receptor antagonists against haloperidol catalepsy is caused by their anticholinergic and antiserotonin properties.
我们研究了苯海拉明、茶苯海明、美吡拉敏(H1受体拮抗剂)和西咪替丁(H2受体拮抗剂)对吗啡、可待因、芬太尼和氟哌啶醇致僵作用的影响。苯海拉明可拮抗镇痛药(尤其是可待因)诱导的僵住症。茶苯海明的拮抗作用较弱(但对可待因诱导的僵住症也非常显著)。美吡拉敏不影响镇痛药诱导的僵住症。所有三种H1受体拮抗剂均减弱了氟哌啶醇诱导的僵住症。脑室内注射西咪替丁不影响镇痛药或氟哌啶醇诱导的僵住症。提示苯海拉明和茶苯海明对镇痛药所致僵住症的拮抗作用与其抗5-羟色胺特性有关,而所有三种H1受体拮抗剂对氟哌啶醇所致僵住症的抗僵住症活性是由其抗胆碱能和抗5-羟色胺特性引起的。