Horváth E J, Palkovits M, Lenkei Z, Gyüre K I, Fekete M I, Arányi P
Institute for Drug Research, H-1325 Budapest, Hungary.
Brain Res Mol Brain Res. 1994 Mar;22(1-4):211-8. doi: 10.1016/0169-328x(94)90049-3.
Homophthalazines (2,3-benzodiazepin-derivates, such as tofisopam, nerisopam, girisopam) constitute a drug family with strong anxiolytic and antipsychotic potencies. By autoradiography, all of these drugs showed a specific distribution pattern of binding sites exclusively in brain areas which relate to the striato-pallido-nigral system, while no specific label was found in any other brain areas in the rat. Quantitative analyses of the autoradiograms by computerized densitometry, as well as by a receptor binding assay on 32 microdissected brain areas showed very high concentrations of tritiated homophthalazines in the glubus pallidus, caudate nucleus, putamen and the substantia nigra. Relatively high density of binding sites was measured in the nucleus accumbens, the olfactory tubercle, the entopeduncular nucleus and the subthalamic nucleus. Concentrations measured in the cerebral cortical areas, cerebellum or brainstem nuclei did not differ from the background. No significant differences were found between the homophthalazines investigated in terms of the distribution patterns or density of binding sites.
高邻苯二氮杂卓类化合物（2,3 - 苯并二氮杂卓衍生物，如托非索泮、奈立索泮、吉立索泮）构成了一类具有强大抗焦虑和抗精神病效力的药物家族。通过放射自显影术，所有这些药物在大脑中仅在与纹状体 - 苍白球 - 黑质系统相关的区域呈现出特异性的结合位点分布模式，而在大鼠的任何其他脑区均未发现特异性标记。通过计算机化密度测定法对放射自显影片进行定量分析，以及对32个显微解剖的脑区进行受体结合测定，结果显示在苍白球、尾状核、壳核和黑质中，氚标记的高邻苯二氮杂卓类化合物浓度极高。在伏隔核、嗅结节、内苍白球核和丘脑底核中测得的结合位点密度相对较高。在大脑皮质区域、小脑或脑干核中测得的浓度与背景值无差异。在所研究的高邻苯二氮杂卓类化合物之间，在结合位点的分布模式或密度方面未发现显著差异。
