Kilian U, Eltze M, Kolassa N
Respiration. 1987;51(1):16-25. doi: 10.1159/000195161.
The antihypertensive drug, urapidil, competitively antagonized the histamine-induced contractions in guinea pig isolated tracheal and ileal preparations. Its affinity to histamine H1-receptors was 3-fold higher than that of histamine but 10- and 30-fold weaker than that of diphenhydramine and indoramin, respectively. Urapidil did not inhibit contractions induced by muscarinic agonists in both organs. Investigations in spontaneously breathing guinea pigs showed a greater efficacy of urapidil than that of diphenhydramine in protecting the animals against histamine-induced bronchospasms, whereas acetylcholine-induced spasms were only moderately inhibited. Theophylline, at a 100-fold higher dosage than urapidil, protected the animals against both histamine and acetylcholine challenges. This experimentally observed effect of urapidil supports clinical trials in hypertensive patients suffering also from obstructive lung disease and/or allergic illness.
抗高血压药物乌拉地尔竞争性拮抗组胺诱导的豚鼠离体气管和回肠标本的收缩。它对组胺H1受体的亲和力比组胺高3倍，但分别比苯海拉明和吲哚拉明弱10倍和30倍。乌拉地尔不抑制这两个器官中由毒蕈碱激动剂诱导的收缩。对自主呼吸的豚鼠的研究表明，乌拉地尔在保护动物免受组胺诱导的支气管痉挛方面比苯海拉明更有效，而乙酰胆碱诱导的痉挛仅受到中度抑制。茶碱的剂量比乌拉地尔高100倍，可保护动物免受组胺和乙酰胆碱的攻击。乌拉地尔的这一实验观察结果支持了对同时患有阻塞性肺病和/或过敏性疾病的高血压患者进行的临床试验。
