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豚鼠和大鼠脑中5-羟色胺4型受体放射性配体结合试验的开发。

Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.

作者信息

Grossman C J, Kilpatrick G J, Bunce K T

机构信息

Pharmacology Division, Glaxo Group Research Ltd., Ware, Herts.

出版信息

Br J Pharmacol. 1993 Jul;109(3):618-24. doi: 10.1111/j.1476-5381.1993.tb13617.x.

DOI:10.1111/j.1476-5381.1993.tb13617.x
PMID:8358562
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2175660/
Abstract
  1. The 5-HT4 receptor antagonist, GR113808, has been radiolabelled to a high specific activity with tritium. 2. Characterization of specific [3H]-GR113808 binding in homogenates of guinea-pig striatum and hippocampus revealed a single site of high affinity (Kd values 0.20 and 0.13 nM respectively). 3. [3H]-GR113808 binding was reversible and displayed rapid kinetics such that association and dissociation were complete within 3 min. 4. Specific [3H]-GR113808 binding was potently and stereoselectively inhibited by agonists and antagonists acting at the 5-HT4 receptor but not by compounds selective for other 5-HT receptors or other neurotransmitter receptors. 5. Autoradiographic analysis revealed a discrete localization in both guinea-pig and rat brain with high concentrations of binding in brain areas such as the striatum, substantia nigra and olfactory tubercle. 6. [3H]-GR113808 binding to homogenates of guinea-pig striatum meets the criteria for labelling of the 5-HT4 receptor and, as such, represents the first characterization of this receptor in a radioligand binding assay.
摘要

  1. 5-羟色胺4（5-HT4）受体拮抗剂GR113808已用氚标记至高比活度。

  2. 对豚鼠纹状体和海马匀浆中特异性[3H]-GR113808结合的表征显示存在一个高亲和力的单一结合位点（解离常数Kd值分别为0.20和0.13纳摩尔）。

  3. [3H]-GR113808结合是可逆的，并表现出快速动力学，结合和解离在3分钟内完成。

  4. 作用于5-HT4受体的激动剂和拮抗剂可有效且立体选择性地抑制特异性[3H]-GR113808结合，但对其他5-HT受体或其他神经递质受体有选择性的化合物则无此作用。

  5. 放射自显影分析显示，在豚鼠和大鼠脑中均有离散定位，在纹状体、黑质和嗅结节等脑区有高浓度结合。

  6. [3H]-GR113808与豚鼠纹状体匀浆的结合符合标记5-HT4受体的标准，因此，这是在放射性配体结合试验中对该受体的首次表征。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1af/2175660/f6b3eb9dc41d/brjpharm00720-0028-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1af/2175660/f6b3eb9dc41d/brjpharm00720-0028-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d1af/2175660/f6b3eb9dc41d/brjpharm00720-0028-a.jpg

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