Magistretti P, Schorderet M
Naunyn Schmiedebergs Arch Pharmacol. 1978 Jun;303(2):189-91. doi: 10.1007/BF00508067.
Benzamides or thioxanthenes were tested as potential antagonists of the cyclic AMP accumulation induced by 10(-4) M dopamine in intact rabbit retinae in vitro in the presence of 5 to 7 mM theophylline. The neuroleptic sulpiride (10(-4) M) was found to be totally inactive whereas a substituted benzamide (clebopride) had small but significant antagonist effect at the same concentration. Among thioxanthenes, isomers of cisconfiguration, which are potent neuroleptics, completely inhibit the cyclic AMP accumulation induced by dopamine, in contrast to trans-isomers which had no inhibitory effects. These data would confirm that retina in vitro is another suitable model for screening antipsychotic activity of classical neuroleptics and that the mechanism of action of sulpiride still needs further investigation.
在5至7 mM茶碱存在的情况下,对苯甲酰胺或噻吨类化合物作为10(-4) M多巴胺在体外完整兔视网膜中诱导的环磷酸腺苷(cAMP)积累的潜在拮抗剂进行了测试。发现抗精神病药物舒必利(10(-4) M)完全无活性,而一种取代苯甲酰胺(氯波必利)在相同浓度下具有微小但显著的拮抗作用。在噻吨类化合物中,顺式构型的异构体是强效抗精神病药物,能完全抑制多巴胺诱导的cAMP积累,而反式异构体则无抑制作用。这些数据将证实体外视网膜是筛选经典抗精神病药物抗精神病活性的另一个合适模型,并且舒必利的作用机制仍需进一步研究。