Arias-Montaño J A, Young J M
Department of Pharmacology, University of Cambridge, UK.
Eur J Pharmacol. 1993 May 15;245(3):291-5. doi: 10.1016/0922-4106(93)90110-u.
The affinities of antagonists at histamine H1 receptors on HeLa cells have been determined from inhibition of histamine-induced inositol phosphate formation in intact and from inhibition of [3H]mepyramine binding to HeLa cell membranes. The dissociation constants of mepyramine and (+)-chlorpheniramine were similar to values for binding to H1 receptors in other mammalian tissues, but much lower than the values reported in an earlier study with [3H]mepyramine and HeLa cell membranes. Evidence is presented that under conditions employed in the earlier study the binding of [3H]mepyramine is largely to secondary, non-H1 receptor sites.
通过抑制组胺诱导的完整HeLa细胞中肌醇磷酸生成以及抑制[3H]美吡拉敏与HeLa细胞膜的结合，已测定了拮抗剂对HeLa细胞上组胺H1受体的亲和力。美吡拉敏和（+）-氯苯那敏的解离常数与它们在其他哺乳动物组织中与H1受体结合的值相似，但远低于早期一项关于[3H]美吡拉敏与HeLa细胞膜研究中报道的值。有证据表明，在早期研究采用的条件下，[3H]美吡拉敏的结合主要是与次要的非H1受体位点。
