Reith M E, Sershen H, Lajtha A
J Neurochem. 1986 Jan;46(1):309-12. doi: 10.1111/j.1471-4159.1986.tb12966.x.
[3H]Cocaine dissociates from its binding sites in the mouse cerebral cortex with a half-time of 25 s. The dissociation kinetics in the striatum is consonant with the presence of two populations of sites with dissociation half times of 2 s and 27 s, comprising 88% and 12%, respectively, of the total binding sites. On the basis of previous pharmacological characterization of [3H]cocaine binding, we propose that the slowly dissociating component represents the sites associated with 5-hydroxytryptamine (serotonin) uptake, and the rapidly dissociating component the 3,4-dihydroxyphenylethylamine (dopamine)-related sites. Evidence is presented that the extremely high dissociation rates do not preclude the measurement of [3H]cocaine binding by rapid filtration. The dissociation of [3H]cocaine from cerebrocortical membranes is slowed to a small but statistically significant extent by serotonin.
[3H]可卡因从其在小鼠大脑皮层的结合位点解离的半衰期为25秒。纹状体中的解离动力学与存在两类结合位点一致，其解离半衰期分别为2秒和27秒，分别占总结合位点的88%和12%。根据先前对[3H]可卡因结合的药理学特征，我们提出缓慢解离成分代表与5-羟色胺（血清素）摄取相关的位点，而快速解离成分代表与3,4-二羟基苯乙胺（多巴胺）相关的位点。有证据表明，极高的解离速率并不妨碍通过快速过滤来测量[3H]可卡因的结合。血清素使[3H]可卡因从脑皮质膜的解离在程度上稍有减慢，但具有统计学意义。
