Ferretti C, Ghi P, Blengio M, Gaietta G, Barrera G, Genazzani E
Istituto di Farmacologia e Terapia Sperimentale, Torino, Italy.
Eur J Pharmacol. 1989 Jul 18;166(2):149-56. doi: 10.1016/0014-2999(89)90054-x.
The ability of tamoxifen, an antiestrogen agent, to antagonise the striatal dopamine receptor hyperactivity induced in rats by chronic treatment with 17 beta-estradiol and 2-hydroxyestradiol or with two receptor blockers (haloperidol and sulpiride) was compared. It was found that tamoxifen antagonised both the increase in [3H]spiperone binding sites and the stereotyped behaviour induced by apomorphine in animals treated with the two steroids but had no effect in animals receiving the two dopamine blockers. These results run counter to the view that introduction of a catechol group in a steroid molecule is of decisive importance in the induction of striatal dopamine receptor hypersensitivity.
比较了抗雌激素药物他莫昔芬拮抗由17β-雌二醇和2-羟基雌二醇或两种受体阻滞剂（氟哌啶醇和舒必利）长期处理诱导的大鼠纹状体多巴胺受体功能亢进的能力。结果发现，他莫昔芬可拮抗两种甾体处理动物中[3H]司哌罗宁结合位点的增加以及阿扑吗啡诱导的刻板行为，但对接受两种多巴胺阻滞剂的动物无影响。这些结果与甾体分子中引入儿茶酚基团对诱导纹状体多巴胺受体超敏反应起决定性作用的观点相悖。
