Kondo M, Taniyama K, Tanaka C
Eur J Pharmacol. 1985 Aug 7;114(1):89-92. doi: 10.1016/0014-2999(85)90526-6.
Histamine H1-receptors were identified in the guinea-pig urinary bladder. Histamine (10(-8)-10(-3) M) produced a dose-dependent contraction which was not altered by either scopolamine or tetrodotoxin. Specific [3H]mepyramine binding to the urinary bladder was saturable and there was a single population of high affinity binding sites with an equilibrium dissociation constant (KD) of 0.77 nM and maximum binding capacity (Bmax) of 68.5 fmol/mg protein. Histamine-induced contraction and [3H]mepyramine binding were inhibited by triploridine, promethazine, d-chlorpheniramine and mepyramine but not by cimetidine. There was a good correlation between mechanical activity and [3H]mepyramine binding as shown by the inhibition affinity constant (Ki) of H1-antagonists. These results provide evidence that the histamine H1-receptor in the guinea-pig urinary bladder is involved in the histamine-induced contraction.
在豚鼠膀胱中鉴定出组胺H1受体。组胺（10⁻⁸ - 10⁻³ M）产生剂量依赖性收缩，东莨菪碱或河豚毒素对此均无影响。膀胱中特异性的[³H]美吡拉敏结合具有饱和性，存在单一的高亲和力结合位点群体，其平衡解离常数（KD）为0.77 nM，最大结合容量（Bmax）为68.5 fmol/mg蛋白质。组胺诱导的收缩和[³H]美吡拉敏结合受到曲普利啶、异丙嗪、右氯苯那敏和美吡拉敏的抑制，但不受西咪替丁的抑制。如H1拮抗剂的抑制亲和力常数（Ki）所示，机械活性与[³H]美吡拉敏结合之间存在良好的相关性。这些结果证明豚鼠膀胱中的组胺H1受体参与了组胺诱导的收缩。
