Mirzoian R S, Seredenin S B, Gan'shina T S, Kostochka L M, Romanycheva N A, Rusakov D Iu
Laboratory of Pharmacology of Cerebrovascular Disorders, Russian Academy of Medical Sciences, Moscow, Russia.
Eksp Klin Farmakol. 1998 May-Jun;61(3):28-31.
The search for serotonin antagonists with cerebrovascular activity was conducted among newly synthesized aromatic and heteroaromatic ethers of tropinone oxim. One of these compounds, namely, hydrochloride-3(3,4,5-trimethoxybenzoiloxiimino-1)-8-methyl-8-a zab icyclo [3,2,1] octane, called tropoxin, prevented the development of serotonin-induced constriction of cerebral vessels in vitro and in vivo experiments. This effect was demonstrated also in experiments with oral administration of the drug. Tropoxin was found to possess affinity for 5-HT2 receptors of the rat brain. Tropoxin surpasses the anti-migraine drug methysergide in antiserotonin cerebrovascular activity. This allows tropoxin to be recommended for study as a means for the treatment of migraine.
在新合成的托品酮肟的芳香族和杂芳香族醚类化合物中寻找具有脑血管活性的血清素拮抗剂。其中一种化合物，即3(3,4,5-三甲氧基苯甲酰氧基亚氨基-1)-8-甲基-8-氮杂双环[3,2,1]辛烷盐酸盐，称为托品辛，在体外和体内实验中均能阻止血清素诱导的脑血管收缩。口服给药实验也证实了这种效果。发现托品辛对大鼠脑的5-HT2受体具有亲和力。托品辛在抗血清素脑血管活性方面超过了抗偏头痛药物麦角酰二乙胺。这使得托品辛有望作为一种治疗偏头痛的药物进行研究。
