ANTAGONISM BY NEUROLEPTICS OF NEUROTRANSMITTER RECEPTORS OF NORMAL HUMAN-BRAIN INVITRO
ANTAGONISM BY NEUROLEPTICS OF NEUROTRANSMITTER RECEPTORS OF NORMAL HUMAN-BRAIN INVITRO
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DOI：
10.1016/0014-2999(84)90478-3
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发表时间：
1984-01-01
影响因子：
5
通讯作者：
NELSON, A
中科院分区：
文献类型：
--
作者：
RICHELSON, E;NELSON, A
使用放射性配体结合技术，测定了一系列精神抑制剂在尸检获得的正常人脑组织的多巴胺（D-2）、毒蕈碱、组胺H1、α 1-和α 2-肾上腺素能受体上的平衡解离常数（KD）。研究了17种不同的化合物在D-2受体和15种化合物在其余的受体。在尾状核的D-2受体，螺哌隆是最有效的化合物（KD = 0.16 nM）;氯氮平的效力最低（KD = 180 nM）。6种化合物在延髓核D-2受体上的KD与它们在尾状核中的KD无显著差异。在其它受体上最有效和最不有效的化合物分别是在毒蕈碱受体上的氯氮平和吗茚酮，在H1受体上的美索达嗪和吗茚酮，在α 1-受体上的螺哌隆和吗茚酮，以及在α 2-受体上的氯氮平和氟哌啶醇。
Using radioligand binding techniques, the equilibrium dissociation constants (KD) were determined for a series of neuroleptics at the dopamine (D-2), muscarinic, histamine H1, .alpha.1- and .alpha.2-adrenergic receptors of normal human brain tissue obtained at autopsy. Seventeen different compounds were studied at the D-2 receptor and 15 compounds at the remaining receptors. At the D-2 receptor of caudate nucleus, spiperone was the most potent compound (KD = 0.16 nM); clozapine the least potent (KD = 180 nM). The KD for 6 compounds at the D-2 receptor of nucleus accumbens were not significantly different from their respective KD in the caudate nucleus. The most potent and least potent compounds at the other receptors were clozapine and molindone at the muscarinic receptor, mesoridazine and molindone at the H1 receptor, spiperone and molindone at the .alpha.1-receptor, and clozapine and haloperidol at the .alpha.2-receptor, respectively.