猫脑干和脊髓中[3H]舒马曲坦结合的放射自显影图谱。

Autoradiographic mapping of [3H]sumatriptan binding in cat brain stem and spinal cord.

作者信息

Mills A, Martin G R

机构信息

Receptor Pharmacology Group, Wellcome Research Laboratories, Beckenham, Kent, UK.

出版信息

Eur J Pharmacol. 1995 Jul 4;280(2):175-8. doi: 10.1016/0014-2999(95)00198-t.

DOI:10.1016/0014-2999(95)00198-t

PMID:7589183

Abstract

In vitro autoradiography was performed on sections of cat brain stem and spinal cord using [3H]sumatriptan. Localization studies using 20-25 nM [3H]sumatriptan showed specific binding to cells in the trigeminal nucleus caudalis and nucleus tractus solitarius of the brain stem and the dorsal horn of the spinal cord. This binding was unaffected by 8-hydroxy-dipropylaminotetralin (20 nM), but was abolished by 5-carboxamidotryptamine (200 nM). Ketanserin displaced total specific binding in the brain stem with a pIC50 of 6.2 but no apparent regional specificity. These results indicate that [3H]sumatriptan labels predominantly 5-HT1D alpha and/or 5-HT1D beta (but not 5-HT1A or 5-HT1F) receptor subtypes in cat brain stem and spinal cord.

摘要

使用[3H]舒马曲坦对猫脑干和脊髓切片进行体外放射自显影。使用20 - 25 nM [3H]舒马曲坦的定位研究表明，其与脑干三叉神经尾侧核、孤束核以及脊髓背角中的细胞存在特异性结合。这种结合不受8 - 羟基 - 二丙基氨基四氢萘（20 nM）的影响，但被5 - 羧基色胺（200 nM）消除。酮色林以6.2的pIC50值取代了脑干中的总特异性结合，但没有明显的区域特异性。这些结果表明，[3H]舒马曲坦在猫脑干和脊髓中主要标记5 - HT1Dα和/或5 - HT1Dβ（而非5 - HT1A或5 - HT1F）受体亚型。