Wright A, Raval P, Eden R J, Owen D A
J Pharmacol Methods. 1987 Sep;18(2):123-9. doi: 10.1016/0160-5402(87)90004-0.
A simple, minimally invasive technique is described which allows assessment of histamine H1-receptor antagonist activity in conscious dogs. The technique is based on the inhibition of the tachycardia caused by intravenous administration of the H1-receptor agonist, 2-pyridylethylamine. The response to 2-pyridylethylamine is dose dependent and is inhibited, in a dose-dependent manner by H1-receptor antagonists, such as temelastine, terfenadine, and chlorpheniramine. In contrast, cimetidine does not inhibit this response. This technique allows comparison of antagonist activity after either oral or intravenous administration of antagonists and also permits an assessment of the time course of antagonism.
本文描述了一种简单的微创技术，该技术可用于评估清醒犬体内组胺H1受体拮抗剂的活性。该技术基于对静脉注射H1受体激动剂2-吡啶乙胺所引起的心动过速的抑制作用。对2-吡啶乙胺的反应呈剂量依赖性，并被H1受体拮抗剂（如特美斯汀、特非那定和氯苯那敏）以剂量依赖的方式抑制。相比之下，西咪替丁不抑制这种反应。该技术可用于比较拮抗剂口服或静脉给药后的拮抗活性，还可评估拮抗作用的时间进程。
