Similarities between the binding of 3H-piflutixol and 3H-flupentixol to rat striatal dopamine receptors in vitro.
Similarities between the binding of 3H-piflutixol and 3H-flupentixol to rat striatal dopamine receptors in vitro.
复制标题
3H-piflutixol 和 3H-flupentixol 与大鼠纹状体多巴胺受体体外结合的相似性。
DOI：
10.1016/0024-3205(81)90150-8
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发表时间：
1981
期刊：
影响因子：
6.1
通讯作者：
J. Hyttel
中科院分区：
文献类型：
--
作者：
J. Hyttel
氚标记的噻吨类神经安定药吡氟噻吨，~ 3 H-PIF与DA受体结合较慢，加入1 μM顺式（Z）-Scatchard分析揭示了0.37 nM的KD和280 fmoles/mg蛋白质（76 pmoles/g湿重）的结合能力。这与3-顺式（Z）-氟哌噻吨（3 H-FPT）结合位点的数目相同，但却是3 H-氟哌啶醇（3 H-HAL）结合位点数目的3倍。抗精神病药可抑制~ 3 H-PIF、~ 3 H-FPT和~ 3 H-HAL的结合以及DA刺激的腺苷酸环化酶活性。氟哌啶醇、螺哌啶醇和匹莫齐特是3 H-PIF和3 H-FPT结合和AC活性的非常弱的抑制剂。氟哌啶醇和阿扑吗啡对~ 3 H-PIF结合的抑制作用的详细分析揭示了两类~ 3 H-PIF结合位点。结果表明，~ 3 H-PIF与~ 3 H-FPT主要结合同一类DA受体。这类D-1受体与AC活性相关，与3 H-HAL标记的受体不同。
The binding of a tritium labelled thioxanthene neuroleptic, piflutixol, to rat striatal membranes in vitro has been characterized.3H-piflutixol (3H-PIF) binds rather slowly to DA receptors.3H-PIF is rather firmly bound to the receptors since after the addition of 1 μM of cis (Z)-flupentixol a half life of 22 min is found. Scatchard analysis reveals a KDof 0.37 nM and a binding capacity of 280 fmoles/mg protein (76 pmoles/g wet weight). This is the same number as3-cis (Z)-flupentixol (3H-FPT) binding sites but three times the number of3H-haloperidol (3H-HAL) binding sites. Neuroleptics inhibit the binding of3H-PIF,3H-FPT and3H-HAL as well as the DA stimulated adenylate cyclase activity. Haloperidol, spiroperidol and pimozide are very weak inhibitors of3H-PIF and3H-FPT binding and of AC activity. A detailed analysis of the inhibition of3H-PIF binding by haloperidol and apomorphine revealed two classes of3H-PIF binding sites. It is concluded that3H-PIF binds predominantly to the same class of DA receptors as does3H-FPT. This class, D-1 receptors, are associated with AC activity and are distinct from those labelled by3H-HAL.