Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro.
Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro.
复制标题
抗精神病药物对正常人脑体外血清素 5-HT1A 和 5-HT2 受体的拮抗作用。
DOI：
10.1016/0014-2999(87)90544-9
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发表时间：
1987
影响因子：
5
通讯作者：
Richelson,E
中科院分区：
文献类型：
--
作者：
Wander,TJ;Nelson,A;Okazaki,H;Richelson,E
利用放射性配体结合技术和人类额叶皮质，我们分别测定了17种神经抑制剂与[3H]WB4101和[3H]酮色林在5-羟色胺5- ht1a和5-羟色胺2受体上的平衡解离常数（KDS）。在5-羟色胺5- ht1a受体上，氯丙噻烯（KD= 230 nM）和氟非那嗪（KD= 40μM）的作用最强和最弱。在5-羟色胺5- ht2受体上，最强和最弱的神经抑制剂分别是spiperone （KD= 0.38 nM）和molindone （KD= 5μM）。
Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDS) of 17 neuroleptics at the serotonin 5-HT1Aand serotonin 5-HT2receptors with [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin 5-HT1Areceptor, the most and least potent neuroleptics were chlorprothixene (KD= 230 nM) and fluphenazine (KD= 40μM), respectively. At the serotonin 5-HT2receptor, the most and least potent neuroleptics were spiperone (KD= 0.38 nM)and molindone, (KD= 5μM), respectively.