组胺H3受体介导抑制豚鼠心肌交感神经末梢去甲肾上腺素释放的直接证据。

Direct evidence for histamine H3 receptor-mediated inhibition of norepinephrine release from sympathetic terminals of guinea pig myocardium.

作者信息

Luo X X, Wen A D, Guo Z A, Tan Y H

机构信息

Department of Pharmacology, Xijing Hospital, Fourth Military Medical University, Xi-an, China.

出版信息

Zhongguo Yao Li Xue Bao. 1996 Sep;17(5):425-8.

PMID:9863165

Abstract

AIM

To study the histamine H3 receptors mediated inhibition of norepinephrine (NE) release from cardiac sympathetic terminals of guinea pig isolated atria.

METHODS

Release of NE induced by electric field stimulation (50 mA, 5 ms) in the bath solution was measured by HPLC-ECD.

RESULTS

The release of NE caused by field stimulation was attenuated by (R)-alpha-methyl-histamine (alpha-MeHA, 0.1 nmol.L-1(-10) mumol.L-1) in a concentration-dependent manner. Thioperamide concentration-dependently antagonized the inhibition of alpha-MeHA. Blockade of H1, H2, alpha 2, beta 2-receptors failed to prevent the inhibitory effect of alpha-MeHA. Thioperamide (1 nmol.L-1(-10) mumol.L-1), when used alone, concentration-dependently facilitated the release of NE evoked by field stimulation.

CONCLUSION

The presynaptic histamine H3-receptors inhibited the NE release from cardiac sympathetic terminals.

摘要

目的

研究组胺H3受体介导的对豚鼠离体心房心脏交感神经末梢去甲肾上腺素（NE）释放的抑制作用。

方法

通过高效液相色谱-电化学检测法（HPLC-ECD）测量浴液中电场刺激（50 mA，5 ms）诱导的NE释放。

结果

（R）-α-甲基组胺（α-MeHA，0.1 nmol·L-1至10 μmol·L-1）以浓度依赖性方式减弱电场刺激引起的NE释放。硫丙拉嗪浓度依赖性地拮抗α-MeHA的抑制作用。阻断H1、H2、α2、β2受体未能阻止α-MeHA的抑制作用。硫丙拉嗪（1 nmol·L-1至10 μmol·L-1）单独使用时，浓度依赖性地促进电场刺激诱发的NE释放。