人红细胞膜中的立体特异性阿片类结合及海洛因成瘾者的变化。
Stereospecific opiate binding in human erythrocyte membranes and changes in heroin addicts.
作者信息
Abood L G, Atkinson G H, MacNeil M
出版信息
J Neurosci Res. 1976;2(5-6):427-31. doi: 10.1002/jnr.490020511.
Stereospecific opiate binding has been demonstrated in human erythrocyte membranes, having a Kd of 9-10(-9) M. In most respects the binding characteristics resemble those of synaptic membranes. These included the correlation of binding affinity and pharmacological potency of opiates; competition by naloxone; inhibition by Ca2+ and Na+; and sensitivity to phospholipases and trypsin. A comparison of stereospecific opiate binding in control human subjects and heroin addicts revealed a 43% increase in the addict group.
已证实在人红细胞膜中存在立体特异性阿片类药物结合，其解离常数（Kd）为9×10⁻⁹ M。在大多数方面，其结合特性类似于突触膜的结合特性。这些特性包括阿片类药物结合亲和力与药理效力的相关性；纳洛酮的竞争性；钙离子（Ca²⁺）和钠离子（Na⁺）的抑制作用；以及对磷脂酶和胰蛋白酶的敏感性。对正常人和海洛因成瘾者的立体特异性阿片类药物结合进行比较后发现，成瘾者组的结合量增加了43%。
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