Todorov S, Zamfirova R
Methods Find Exp Clin Pharmacol. 1986 Dec;8(12):705-9.
The role of the H1- and H2-receptors in the modulatory effects of histamine and other histaminergic drugs on smooth muscle adrenergic neurotransmission was studied on isolated preparations from rat vas deferens. The typical biphasic action (potentiation by low concentrations and inhibition by high concentrations) of histamine and some H1- or H2-agonists on vas deferens contractions induced by low frequency electrical stimulation (ES) was markedly changed by H1- or H2-antagonists. After blockade of H1-receptors, the potentiating effect of histamine and the histaminergic agonists was diminished or even reversed. The inhibition of the smooth muscle contractions by the drugs tested was stronger after H1-antagonists. Blockade of H2-receptors usually enhanced the potentiating effect of the histaminergic agonists on ES-evoked vas deferens contractions. The inhibitory action of histamine and the histaminergic agents tested was decreased or even reversed after H2-receptor blockade. These results confirm the presence of H1-excitatory and H2-inhibitory receptors whose activation or inhibition can modulate adrenergic neurotransmission in vas deferens.
在大鼠输精管的离体标本上,研究了H1和H2受体在组胺及其他组胺能药物对平滑肌肾上腺素能神经传递的调节作用中的角色。组胺及一些H1或H2激动剂对低频电刺激(ES)诱导的输精管收缩的典型双相作用(低浓度增强,高浓度抑制)被H1或H2拮抗剂显著改变。阻断H1受体后,组胺及组胺能激动剂的增强作用减弱甚至逆转。H1拮抗剂作用后,受试药物对平滑肌收缩的抑制作用更强。阻断H2受体通常增强组胺能激动剂对ES诱发的输精管收缩的增强作用。H2受体阻断后,组胺及受试组胺能药物的抑制作用减弱甚至逆转。这些结果证实了存在H1兴奋性受体和H2抑制性受体,其激活或抑制可调节输精管中的肾上腺素能神经传递。