用[3H]美吡拉敏鉴定豚鼠气道中组胺H1受体的分布及特征

Distribution and characteristics of histamine H1-receptors in guinea-pig airways identified by [3H]mepyramine.

作者信息

Carswell H, Nahorski S R

出版信息

Eur J Pharmacol. 1982 Jul 9;81(2):301-7. doi: 10.1016/0014-2999(82)90448-4.

Abstract

The distribution and characteristics of histamine H1-receptors in various regions of guinea-pig airways have been studied using the antagonist [3H]mepyramine. A similar density of specific [3H]mepyramine sites was found in trachea, bronchi and parenchyma and these sites possessed pharmacological properties expected of a histamine H1-receptor. In addition, there was a large component of [3H]mepyramine binding that did not show stereoselectivity towards the isomers of chlorpheniramine and as such cannot be considered to represent binding to an H1-receptor. This non-specific component accounted for approximately 80% of total [3H]mepyramine binding when assays were performed in Tris-HCl buffer but was considerably reduced by the presence of sodium ions in the incubation buffer. The present results do not confirm previous reports on the heterogeneity of histamine H1-receptors in guinea-pig lung and suggest that this may, in part, be due to difficulties in accurately assessing true receptor specific binding.

摘要

使用拮抗剂[³H]美吡拉敏研究了豚鼠气道各区域组胺H1受体的分布和特性。在气管、支气管和实质中发现了相似密度的特异性[³H]美吡拉敏位点，这些位点具有组胺H1受体预期的药理学特性。此外，[³H]美吡拉敏结合中有很大一部分对氯苯那敏异构体不表现出立体选择性，因此不能认为代表与H1受体的结合。当在Tris-HCl缓冲液中进行测定时，这种非特异性成分约占总[³H]美吡拉敏结合的80%，但孵育缓冲液中存在钠离子时，该成分会显著减少。目前的结果不支持先前关于豚鼠肺中组胺H1受体异质性的报道，并表明这可能部分是由于准确评估真正的受体特异性结合存在困难。