Hoss W, Reese J H, Smiley C
J Neurosci Res. 1977;3(4):257-66. doi: 10.1002/jnr.490030403.
The intrinsic fluorescence of apomorphine has been used to measure its binding to neural membranes. A large number of relatively weak binding sites are concentrated in myelin and synaptic membrane fractions. Butyrophenones have the highest affinities for these sites--KD = 43 micrometer for haloperidol--while dopamine and dopamine releasers and reuptake blockers, as well as a variety of other alkaloids, have much lower affinities. The sites are hydrophobic and undergo a phase transition to a highly fluid state near 26 degrees C. Calcium is a noncompetitive inhibitor of apomorphine binding. Some of the actions of neuroleptic drugs may result from binding to these hydrophobic membrane sites in vivo, blocking conduction in small catecholamine axons.
阿扑吗啡的固有荧光已被用于测定其与神经膜的结合。大量相对较弱的结合位点集中在髓磷脂和突触膜组分中。丁酰苯类药物对这些位点具有最高的亲和力——氟哌啶醇的解离常数KD = 43微摩尔——而多巴胺、多巴胺释放剂和再摄取阻滞剂以及各种其他生物碱的亲和力则低得多。这些位点具有疏水性，在接近26摄氏度时会发生相变，转变为高流动性状态。钙是阿扑吗啡结合的非竞争性抑制剂。抗精神病药物的一些作用可能是由于在体内与这些疏水膜位点结合，阻断了小的儿茶酚胺轴突中的传导。
