Danchev N D, Rozhanets V V, Zhmurenko L A, Glozman O M, Zagorevskiĭ V A
Biull Eksp Biol Med. 1984 May;97(5):576-8.
The differences in the pharmacological effects of R(+)- and S(-)-isomers of the atypical antidepressant viloxazin were discovered in two behavioral models. The S(-)-isomer appeared 5 times as active as the R(+)-isomer under acute administration. In chronic administration, (15 days), the R(+)-isomer appeared ineffective. Comparison of the affinity of the racemate, R(+) and S(-)-isomers for alpha 1-, alpha 2- and beta-adrenoreceptors, as well as for serotonin, C1, benzodiazepine, imipramine and dopamine receptors did not demonstrate any stereospecificity of viloxazin isomers. It is assumed that some other receptors (histamine, acetylcholine) present the targets for the pharmacological action of viloxazin or the latter one has, like zimelidin , specific binding sites of its own.
在两种行为模型中发现了非典型抗抑郁药维洛沙嗪的R(+)-和S(-)-异构体在药理作用上的差异。急性给药时,S(-)-异构体的活性似乎是R(+)-异构体的5倍。在慢性给药(15天)时,R(+)-异构体似乎无效。消旋体、R(+)和S(-)-异构体对α1-、α2-和β-肾上腺素能受体以及5-羟色胺、C1、苯二氮䓬、丙咪嗪和多巴胺受体的亲和力比较未显示维洛沙嗪异构体有任何立体特异性。据推测,其他一些受体(组胺、乙酰胆碱)是维洛沙嗪药理作用的靶点,或者后者像齐美利定一样有其自身的特异性结合位点。