DISTRIBUTION AND CHARACTERIZATION OF THE [H-3] GRANISETRON-LABELED 5-HT3 RECEPTOR IN THE HUMAN FOREBRAIN
DISTRIBUTION AND CHARACTERIZATION OF THE [H-3] GRANISETRON-LABELED 5-HT3 RECEPTOR IN THE HUMAN FOREBRAIN
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DOI：
10.1016/0028-3908(93)90027-z
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发表时间：
1993-12-01
影响因子：
4.7
通讯作者：
BARNES, NM
中科院分区：
文献类型：
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作者：
BUFTON, KE;STEWARD, LJ;BARNES, NM
本研究证明了[H-3]格拉司琼标记的5-HT 3受体在人类前脑中的分布，其中海马、尾状核、壳核、伏核和杏仁核的匀浆中该受体的水平相对较高。在其他脑区和颈迷走神经中发现较低水平的5-HT受体。在人壳核匀浆中标记的5-HT 3受体的药理学表征鉴定出与NG 108 -15神经母细胞瘤-神经胶质瘤细胞匀浆中的5-HT 3受体相比，d-筒箭毒碱的亲和力相对较低。相反，在这两种制剂中，19种其他5-HT受体配体对[H-3]格拉司琼标记受体的亲和力没有显著差异。这些发现表明，人壳核5-HT 3接受独特的药理学，当在疾病的动物模型中评估时，考虑到所报道的对该受体有活性的化合物的临床潜力，这可能具有重要意义。
The present study has demonstrated the distribution of [H-3]granisetron-labelled 5-HT3, receptors in the human forebrain with relatively high levels of this receptor in homogenates of hippocampus, caudate nucleus, putamen, nucleus accumbens and amygdala. Lower levels of 5-HT, receptors were found in other brain regions and the cervical vagus nerve. Pharmacological characterization of the labelled 5-HT3, receptor in human putamen homogenates identified a relatively low affinity for d-tubocurarine compared to the 5-HT, receptor in NG108-15 neuroblastoma-glioma cell homogenates. In contrast, the affinities of 19 other 5-HT, receptor ligands were not significantly different for the [H-3]granisetron-labelled receptor in these two preparations. Such findings indicate that the human putamen 5-HT3 recep a unique pharmacology which may have significance given the reported clinical potential of compounds active at this receptor when assessed in animal models of disease.