Arborelius L, Höök B B, Hacksell U, Svensson T H
Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden.
J Neural Transm Gen Sect. 1994;96(3):179-86. doi: 10.1007/BF01294785.
(S)-UH-301 [(S)-5-fluoro-8-hydroxy-2-(dipropylamino)-tetralin, 0.5-4.0 mg/kg i.v.] did not significantly alter the firing rate of 5-hydroxytryptamine (5-HT) containing neurons in the dorsal raphe nucleus (DRN) as a group, although some individual cells were activated whereas others were depressed. However, (S)-UH-301 (2.0 mg/kg i.v.) consistently reversed the inhibition of DRN-5-HT cells produced by the selective 5-HT1A receptor agonist (R)-8-OH-DPAT (0.5 microgram/kg i.v.) and the dose-response curve for this effect of (R)-8-OH-DPAT was markedly shifted to the right by pretreatment with (S)-UH-301 (1.0 mg/kg i.v.). These results support the notion that (S)-UH-301 acts as an antagonist at central 5-HT1A receptors.
(S)-UH-301[（S）-5-氟-8-羟基-2-（二丙基氨基）四氢萘，静脉注射0.5-4.0毫克/千克]作为一个整体，并没有显著改变中缝背核（DRN）中含5-羟色胺（5-HT）神经元的放电频率，尽管一些单个细胞被激活，而另一些则受到抑制。然而，(S)-UH-301（静脉注射2.0毫克/千克）持续逆转了选择性5-HT1A受体激动剂(R)-8-羟基二丙胺四氢萘（静脉注射0.5微克/千克）对DRN-5-HT细胞的抑制作用，并且(R)-8-羟基二丙胺四氢萘这种作用的剂量反应曲线通过(S)-UH-301（静脉注射1.0毫克/千克）预处理而明显右移。这些结果支持了(S)-UH-301作为中枢5-HT1A受体拮抗剂的观点。
