Noble E P, Bommer M, Sincini E, Costa T, Herz A
Biochem Biophys Res Commun. 1986 Mar 13;135(2):566-73. doi: 10.1016/0006-291x(86)90031-8.
Adrenal medullary chromaffin cells maintained in vitro were prelabeled with [3H]inositol and the accumulation of [3H]inositol-1-phosphate, was determined following stimulation with a variety of pharmacological agents. Carbachol, bradykinin, and histamine produced significantly greater accumulation of [3H] inositol-1-phosphate over basal levels, with histamine producing the greatest effect. H1-histamine receptor antagonists, mepyramine, pyrilamine, tripelennamine and clemastine were all able to reduce or completely block the histamine response. The two specific H2-histamine receptor antagonists, cimetidine and ranitidine, had no effect on this response. Histamine dose-response characteristics in the presence of mepyramine and clemastine suggest the H1 antagonism to be competitive in nature.
体外培养的肾上腺髓质嗜铬细胞先用[3H]肌醇预标记,然后在多种药理剂刺激后测定[3H]肌醇-1-磷酸的积累。卡巴胆碱、缓激肽和组胺使[3H]肌醇-1-磷酸的积累比基础水平显著增加,其中组胺的作用最大。H1组胺受体拮抗剂美吡拉敏、吡苄明、曲普利啶和氯马斯汀都能够降低或完全阻断组胺反应。两种特异性H2组胺受体拮抗剂西咪替丁和雷尼替丁对该反应无影响。在存在美吡拉敏和氯马斯汀的情况下组胺的剂量反应特征表明H1拮抗作用本质上是竞争性的。