Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro.
Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro.
复制标题
抗抑郁药对正常人脑体外血清素 S1 和 S2 受体的拮抗作用。
DOI：
10.1016/0014-2999(86)90596-0
复制
发表时间：
1986
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
Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDs) of 25 antidepressants at the serotonin S1(probably the S1Asubtype) and serotonin S2receptors using [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin S1receptor, the most and least potent antidepressants were trazodone (KD= 60 nM) and bupropion (KD= 170μM), respectively. At the serotonin S2receptor, the most and least potent antidepressants were amoxapine (KD= 0.6 nM) and bupropion (KD= 90μM), respectively. Analysis of the data revealed a relationship between structure and serotonin S1affinity for some tricyclic antidepressants. Buspirone, a new anxiolytic agent, possessed high affinity for the serotonin S1receptor (KD= 3.8 nM).
