Akiyama Y, Kamei C, Tasaka K
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Methods Find Exp Clin Pharmacol. 1990 Sep;12(7):457-65.
The effects of histamine (Hi) and related compounds on rat mesenterial adipocytes were investigated using electrophysiological techniques. Hi caused a concentration-related depolarization and significant effect was observed at concentrations higher than 5 x 10(-6) M. Effective membrane resistance was also decreased by Hi. The H1-agonists 2-methylHi and 2-thiazolylethylamine caused no depolarization even at a concentration of 5 x 10(-4) M, but the H2-agonists, 4-methylHi and impromidine decreased resting membrane potentials. While 4-methylHi was less potent than Hi, impromidine was more potent. The H1-antagonists diphenhydramine and pyrilamine did not affect Hi-induced depolarization. However, H2-antagonists like cimetidine and ranitidine caused a significant inhibition even at a concentration of 10(-6) M. As in the case of isoproterenol, the decrease in resting membrane potentials induced by Hi was significantly potentiated by theophylline. Dibutyryl cyclic AMP treatment and intracellular application of cyclic AMP also caused a marked depolarization.
使用电生理技术研究了组胺（Hi）及相关化合物对大鼠肠系膜脂肪细胞的影响。Hi引起浓度相关的去极化，且在高于5×10⁻⁶ M的浓度下观察到显著效应。Hi还降低了有效膜电阻。H1激动剂2-甲基Hi和2-噻唑基乙胺即使在5×10⁻⁴ M的浓度下也未引起去极化，但H2激动剂4-甲基Hi和英普咪定降低了静息膜电位。虽然4-甲基Hi的效力低于Hi，但英普咪定的效力更强。H1拮抗剂苯海拉明和吡苄明不影响Hi诱导的去极化。然而，H2拮抗剂如西咪替丁和雷尼替丁即使在10⁻⁶ M的浓度下也会引起显著抑制。与异丙肾上腺素的情况一样，茶碱显著增强了Hi诱导的静息膜电位降低。二丁酰环磷酸腺苷处理和细胞内应用环磷酸腺苷也引起明显的去极化。
