Möhler H, Okada T
Br J Psychiatry. 1978 Sep;133:261-8. doi: 10.1192/bjp.133.3.261.
Benzodiazepines bind with high affinity to a specific benzodiazepine receptor, which occurs exclusively in the central nervous system. The affinity of various benzodiazepines to the receptor closely parallels their pharmacological and therapeutic potency. Binding to the receptor is stereospecific. The receptor is mainly localized in the synaptic membrane fraction and has its highest density in cortical areas of the brain. In Huntington's chorea a decrease in benzodiazepine receptor binding is found in caudate nucleus and putamen, which, at least in putamen, is due to a loss of benzodiazepine receptors apparently located on GABA neurones, which degenerate in Huntington's chorea. The loss of benzodiazepine receptors might explain why the ameliorative effects of benzodiazepines in the early stages of the disease are not sustained in the later stages.
苯二氮䓬类药物以高亲和力与特定的苯二氮䓬受体结合，该受体仅存在于中枢神经系统中。各种苯二氮䓬类药物对该受体的亲和力与其药理和治疗效力密切相关。与受体的结合具有立体特异性。该受体主要定位于突触膜部分，在大脑皮质区域密度最高。在亨廷顿舞蹈病中，尾状核和壳核中苯二氮䓬受体结合减少，至少在壳核中，这是由于明显位于GABA神经元上的苯二氮䓬受体丧失所致，这些神经元在亨廷顿舞蹈病中发生退化。苯二氮䓬受体的丧失可能解释了为什么苯二氮䓬类药物在疾病早期的改善作用在后期不能持续。
