Holoubek G, Müller W E
Department of Pharmacology, Biocenter University Frankfurt, Frankfurt, Germany.
J Neural Transm (Vienna). 2003 Oct;110(10):1169-79. doi: 10.1007/s00702-003-0019-5.
The atypical anxiolytic and antidepressive drug opipramol binds with high affinity to sigma1 and somewhat lower affinity to sigma2 sites. After subchronic treatment, opipramol significantly down-regulated sigma2 but not sigma1 sites. This effect was not seen for imipramine, citalopram, and reboxetine under similar conditions. On the other hand, only imipramine reduced the number of sigma1 sites. It is suggested that effects at sigma2 sites are involved in the anxiolytic properties of opipramol.
非典型抗焦虑和抗抑郁药物奥匹哌醇与σ1位点具有高亲和力，与σ2位点的亲和力略低。亚慢性治疗后，奥匹哌醇显著下调σ2位点，但对σ1位点无此作用。在类似条件下，丙咪嗪、西酞普兰和瑞波西汀未出现这种效应。另一方面，只有丙咪嗪减少了σ1位点的数量。有人提出，对σ2位点的作用与奥匹哌醇的抗焦虑特性有关。
