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组胺H_3受体定位于心交感神经末梢突触前膜的进一步证明

Further evidence for the presynaptic location of histamine H-3-recep-tors on sympathetic terminals of guinea pig myocardium
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摘要 目的:观察[ ̄3H]组胺在心肌细胞粗制膜上的结合情况.方法:制备心肌细胞粗制膜,将膜制备与[ ̄3H]组胺在37℃下共同孵育30min,然后将孵育液经玻璃纤维膜减压抽滤.滤膜烘干后放入闪烁瓶中,记录放射活性.结果:选择性H-3受体激动剂α-甲基组胺(α-MeHA,1μmol/L)可竞争性抑制[ ̄3H]组胺在心肌膜制备上的特异性结合,[ ̄3H]组胺(0.5和1 nmol/L)特异性结合量减少至对照值的64.1±11.1%和60.51±4.1%。6-羟基多巴胺(6-OHDA)化学切割交感神经后,可以使[ ̄3H]组胺与膜受体的结合量减少至对照值的77.3±6.9%和80.1±6.9%.在化学去交感神经的膜制备中,α-MeHA仅轻度降低组胺与膜受体的特异性结合量.结论:化学法切除交感神经后,丢失了一部分与[ ̄3H]组胺结合的受体蛋白,这部分定位于交感神经末梢的组胺受体,可以被α-MeHA竞争性结合,属于组胺H-3受体. objective :To observe the specific binding of[ ̄H]histamine on the membrane fraction of guinea pig myocardium following chemical sympathectomy by 6-hydroxydopamine. Metkod :The isolated guinea pig heart was homogenized and membrane fraction of myocardium was incubated with[ ̄3H]histamine for 30 minat 37℃. Then incubated fluid received rapid filtration over glass fiber filter and after dried ,filter membrane was placed in a scintillator so as to measure radioactivity by liquid scintillation spectrometry. Results : Selec-tive H-3-receptor agonist α-methylhistamine (α-MeHA, 1 μmol /L)could competitively inhibit the specific binding of[ ̄3H]histamine on the membrane fraction of myocardium , which decreased the specific binding quantity to 64.1±11.1%and 60. 5±4.1%of control values respectively when the concentrations of[ ̄3H]his-tamine were 0.5 and 1 nmol/L. Chemical sympathectomy by 6-OHDA could bring the specific binding quanti-ty between histamine and membrane receptors down to 77.3±6. 9 and 80.1±6.9%of control values. While α-MeHA caused only slight drop of the specific binding between histamine and membrane fractiion treated by sympathectomy. Conclusion :Chemical sympathectomy can give riseto loss of some presynaptic binding sites(or receptors) of[ ̄3H]Hihistamine located on sympathetic nerve terminals. α-MeHA can combine competitively with these histamine receptors so they might be H-3-subtype of histamine receptors.
出处 《第四军医大学学报》 1995年第5期324-327,共4页 Journal of the Fourth Military Medical University
关键词 心肌 交感神经末梢 突触 组胺H3受体 受体 histamine H-3-receptors (R)-α -methylhistamine [ ̄3H]histamine myocardium
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参考文献2

  • 1罗晓星,Asia-Pacific J Pharmacol,1993年,8卷,17页 被引量:1
  • 2罗晓星,Eur J Pharmacol,1991年,204卷,311页 被引量:1

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