Maj J, Sarnek J, Klimek V, Rawlów A
Pharmacol Biochem Behav. 1976 Aug;5(2):201-5. doi: 10.1016/0091-3057(76)90037-x.
The anticataleptic action of cyproheptadine, a tricyclic compound known as antiserotonin, anticholinergic and antihistaminic drug in comparison to that of atropine, promethazine, imipramine, desipramine, chlorimipramine and nomifensine was studied in rats. The catalepsy induced by spiperon, pimozide or fluphenazine was antagonized by cyproheptadine, atropine and promethazine. Imipramine and nomifensine were less active, desipramine and chlorimipramine without effect. The reserpine- and alpha-methyltyrosine-catalepsy was counteracted by cyproheptadine, promethazine and nomifensine, but not by atropine or tricyclic antidepressants. Only cyproheptadine and promethazine antagonized the catalepsy caused by a combined treatment with reserpine and alpha-methyltyrosine. The pilocarpine-catalepsy was abolished by atropine, promethazine and nomifensine and unaffected by tricyclic antidepressants. Atropine and promethazine antagonized also the physostigmine-catalepsy. The catalepsy induced by both cholinomimetic drugs was not changed or increased by cyproheptadine. The results presented indicate that cyproheptadine differs in its anticataleptic activity from all the drugs used for comparison. Possible mechansims of this activity are discussed.
在大鼠中,研究了赛庚啶(一种已知具有抗血清素、抗胆碱能和抗组胺作用的三环化合物)与阿托品、异丙嗪、丙咪嗪、地昔帕明、氯米帕明和诺米芬辛相比的抗僵住作用。赛庚啶、阿托品和异丙嗪可拮抗由舒必利、匹莫齐特或氟奋乃静诱导的僵住症。丙咪嗪和诺米芬辛的活性较低,地昔帕明和氯米帕明则无作用。赛庚啶、异丙嗪和诺米芬辛可对抗利血平和α-甲基酪氨酸诱导的僵住症,但阿托品或三环类抗抑郁药则不能。只有赛庚啶和异丙嗪可拮抗利血平和α-甲基酪氨酸联合治疗引起的僵住症。毛果芸香碱诱导的僵住症可被阿托品、异丙嗪和诺米芬辛消除,不受三环类抗抑郁药影响。阿托品和异丙嗪也可拮抗毒扁豆碱诱导的僵住症。赛庚啶对两种拟胆碱药诱导的僵住症无影响或使其增强。所呈现的结果表明,赛庚啶的抗僵住活性与所有用于比较的药物不同。讨论了这种活性可能的机制。