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进一步的证据表明,3H-顺式(Z)氟哌噻吨与大鼠纹状体中与腺苷酸环化酶相关的多巴胺受体(D-1)结合。

Further evidence that 3H-cis(Z)flupenthixol binds to the adenylate cyclase-associated dopamine receptor (D-1) in rat corpus striatum.

作者信息

Hyttel J

出版信息

Psychopharmacology (Berl). 1980 Jan;67(1):107-9. doi: 10.1007/BF00427604.

Abstract

The proposal that 3H-cis(Z)flupenthixol (3H-FPT) preferentially binds to striatal dopamine receptors associated with adenylate cyclase activity (D-1), distinct from dopamine receptors to which 3H-haloperidol (3H-hal) binds (D-2), has been investigated further. The dopamine agonists bromocriptine and ergotamine were 60-times more potent as displacers of 3H-hal than 3H-FPT binding. Other dopamine agonists (ergometrine, dopamine, apomorphine, 2-amino-6,7-dihydroxy-tetralin (ADTN), and ergocornine) also shared this profile, although a smaller ratio was found for these compounds. Substituted benzamides (clebopride greater than sultopride greater than sulpiride greater than metoclorpramide greater than tiapride) displace 3H-hal but have only a very slight displacing effect towards 3H-FPT, and did not inhibit dopamine-stimulated adenylate cyclase activity. The same pattern is shared by oxiperomide and molindone. Together, these results support the idea that 3H-FPT labels another class of dopamine receptors than does 3H-hal, and that the former class most likely is associated with adenylate cyclase.

摘要

3H-顺式(Z)氟哌噻吨(3H-FPT)优先结合与腺苷酸环化酶活性相关的纹状体多巴胺受体(D-1),这与3H-氟哌啶醇(3H-hal)所结合的多巴胺受体(D-2)不同,这一观点已得到进一步研究。多巴胺激动剂溴隐亭和麦角胺作为3H-hal结合的置换剂,其效力比作为3H-FPT结合的置换剂高60倍。其他多巴胺激动剂(麦角新碱、多巴胺、阿扑吗啡、2-氨基-6,7-二羟基四氢萘(ADTN)和麦角隐亭)也具有这种特性,尽管这些化合物的比例较小。取代苯甲酰胺(氯波必利>舒托必利>舒必利>甲氧氯普胺>替阿普明)可置换3H-hal,但对3H-FPT只有非常轻微的置换作用,且不抑制多巴胺刺激的腺苷酸环化酶活性。奥昔哌隆和吗茚酮也有相同的模式。总之,这些结果支持这样一种观点,即3H-FPT标记的多巴胺受体类别与3H-hal不同,且前一类受体很可能与腺苷酸环化酶有关。

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