从组胺H_3受体的配体开发新药的展望

The histamine H_3 receptor ligands: potential therapeutic uses

近年通过克隆技术鉴定了组胺H3和H4亚型受体。H3受体是突触前受体,其功能为调节组胺的生物合成与从末梢释放。在其他神经元也有H3受体的存在,因而还能调节其他若干神经递质的释放。已经发现了一些H3受体的激动剂与拮抗剂。实验研究表明这些激动剂与拮抗剂有广泛的生物作用。迄今尚未有这类化合物经批准在临床应用,但从其功用来日可能开发出一些有效药物。

A third histamine receptor subtype was characterized in recent years. The H 3 receptors are presynaptic receptors which regulate the synthesis and release of histamine in histaminergic neurons in central nervous system. The subtype receptors also appear to occur on nonhistaminergic axon terminals, regulating release of other important neurotransmitters. Various agonists and antagonists of the subtype are reviewed. So far there have not been H 3 receptor ligands in therapeutic uses. However, a wide range of central effects following H 3 receptor stimulation or blockade has been described by various experimental studies. It is hoped that some novel histaminergic drugs will be developed in the future. [