组胺对豚鼠离体心房中[3H]-去甲肾上腺素静息释放及刺激诱导释放的影响。
Effects of histamine on the resting and stimulation-induced release of [3H]-noradrenaline in guinea-pig isolated atria.
作者信息
Rand M J, Story D F, Wong-Dusting H K
出版信息
Br J Pharmacol. 1982 Jan;75(1):57-64. doi: 10.1111/j.1476-5381.1982.tb08757.x.
Abstract
1 The sympathetic transmitter stores of guinea-pig isolated atria were labelled with [3H]-noradrenaline. The effects of histamine (0.3 to 100 mumol/l) on resting and stimulation-induced (S-I, 2 Hz for 10 s) release of radioactivity were investigated. 2 Histamine, in low concentrations (0.3 and 1 mumol/l) had no effect on resting release but inhibited S-I release of radioactivity. The inhibition was abolished by the H2-receptor antagonist, cimetidine (10 mumol/l) and also by the H1-receptor antagonist, mepyramine (1 mumol/l). 3 The inhibitory actions of histamine on S-I release were not due to indirect effects involving alpha-adrenoceptors, beta-adrenoceptors, muscarinic cholinoceptors or prostaglandin synthesis. 4 Histamine in a high concentration (100 mumol/l) increased the resting and S-I release of radioactivity. The increase in resting release was abolished by the neuronal uptake blocking drug cocaine (30 mumol/l) but the increase in S-I release was only partially blocked by cocaine.
摘要
用[3H] - 去甲肾上腺素标记豚鼠离体心房的交感递质储存部位。研究了组胺（0.3至100μmol / l）对静息和刺激诱导（S - I，2Hz，持续10秒）放射性物质释放的影响。
低浓度（0.3和1μmol / l）的组胺对静息释放无影响，但抑制放射性物质的S - I释放。H2受体拮抗剂西咪替丁（10μmol / l）和H1受体拮抗剂美吡拉敏（1μmol / l）均可消除这种抑制作用。
组胺对S - I释放的抑制作用并非由于涉及α - 肾上腺素能受体、β - 肾上腺素能受体、毒蕈碱胆碱能受体或前列腺素合成的间接作用。
高浓度（100μmol / l）的组胺增加了放射性物质的静息和S - I释放。静息释放的增加被神经元摄取阻断药物可卡因（30μmol / l）消除，但S - I释放的增加仅被可卡因部分阻断。
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