Wander T J, Nelson A, Okazaki H, Richelson E
Eur J Pharmacol. 1986 Dec 16;132(2-3):115-21. doi: 10.1016/0014-2999(86)90596-0.
Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDs) of 25 antidepressants at the serotonin S1 (probably the S1A subtype) and serotonin S2 receptors using [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin S1 receptor, the most and least potent antidepressants were trazodone (KD = 60 nM) and bupropion (KD = 170 microM), respectively. At the serotonin S2 receptor, the most and least potent antidepressants were amoxapine (KD = 0.6 nM) and bupropion (KD = 90 microM), respectively. Analysis of the data revealed a relationship between structure and serotonin S1 affinity for some tricyclic antidepressants. Buspirone, a new anxiolytic agent, possessed high affinity for the serotonin S1 receptor (KD = 3.8 nM).
利用放射性配体结合技术和人类额叶皮质，我们分别使用[3H]WB4101和[3H]酮色林测定了25种抗抑郁药在5-羟色胺S1（可能是S1A亚型）和5-羟色胺S2受体上的平衡解离常数（KDs）。在5-羟色胺S1受体上，效力最强和最弱的抗抑郁药分别是曲唑酮（KD = 60 nM）和安非他酮（KD = 170 microM）。在5-羟色胺S2受体上，效力最强和最弱的抗抑郁药分别是阿莫沙平（KD = 0.6 nM）和安非他酮（KD = 90 microM）。数据分析揭示了某些三环类抗抑郁药的结构与5-羟色胺S1亲和力之间的关系。新型抗焦虑药丁螺环酮对5-羟色胺S1受体具有高亲和力（KD = 3.8 nM）。
