In vivo binding of 3H-pimozide in mouse striatum: effects of dopamine agonists and antagonists.
In vivo binding of 3H-pimozide in mouse striatum: effects of dopamine agonists and antagonists.
复制标题
小鼠纹状体中 3H-匹莫齐特的体内结合：多巴胺激动剂和拮抗剂的作用。
DOI：
10.1016/0024-3205(77)90116-3
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发表时间：
1977
期刊：
影响因子：
6.1
通讯作者：
J. Schwartz
中科院分区：
文献类型：
--
作者：
M. Baudry;M. Martres;J. Schwartz
有几条证据表明，静脉注射3 H-匹莫齐特可导致抗精神病药与多巴胺能受体的特异性体内结合。首先，与小脑等非多巴胺能结构相比，3 H-匹莫齐特优先蓄积在纹状体。第二，3 H-匹莫齐特的选择性蓄积可通过预先给药各种抗精神病药以及阿扑吗啡来防止。此外，拮抗剂的剂量，防止这种积累是相同的，导致纹状体HVA水平的增加。第三，3 H-匹莫齐特的积累并不被各种非多巴胺能药物所改变，然而，3 H-匹莫齐特的结合并不被间接多巴胺激动剂所阻止，甚至在高剂量时被d-苯丙胺大大增加。直接或间接的多巴胺激动剂可能有利于通过受体位点的修饰的拮抗剂的结合的可能性进行了讨论。
Several lines of evidence indicate that the i.v. injection of3H-pimozide results in a specific in vivo binding of the neuroleptic to dopaminergic receptors.First,3H-pimozide is preferentially accumulated in the striatum as compared to non-dopaminergic structures like the cerebellum. Second, the selective accumulation of3H-pimozide is prevented by prior administration of various neuroleptics as well as by apomorphine. Moreover, doses of antagonists which prevent this accumulation were identical to those which lead to an increased striatal HVA level. Third,3H-pimozide accumulation is not modified by the administration of a variety of non-dopaminergic agents.However,3H-pimozide binding is not prevented either by indirect dopamine agonists and is even greatly increased by d-amphetamine at high doses. The possibility that direct or indirect dopamine agonists may favour the binding of the antagonist through a modification of receptor sites is discussed.