组胺H3受体：从基因克隆到H3受体药物

The histamine H3 receptor: from gene cloning to H3 receptor drugs.

作者信息

Leurs Rob, Bakker Remko A, Timmerman Henk, de Esch Iwan J P

机构信息

Division of Medicinal Chemistry, Leiden/Amsterdam Center for Drug Research, Vrije Universiteit Amsterdam, Faculty of Science, de Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.

出版信息

Nat Rev Drug Discov. 2005 Feb;4(2):107-20. doi: 10.1038/nrd1631.

DOI:10.1038/nrd1631

PMID:15665857

Abstract

Since the cloning of the histamine H(3) receptor cDNA in 1999 by Lovenberg and co-workers, this histamine receptor has gained the interest of many pharmaceutical companies as a potential drug target for the treatment of various important disorders, including obesity, attention-deficit hyperactivity disorder, Alzheimer's disease, schizophrenia, as well as for myocardial ischaemia, migraine and inflammatory diseases. Here, we discuss relevant information on this target protein and describe the development of various H(3) receptor agonists and antagonists, and their effects in preclinical animal models.

摘要

自1999年洛文伯格及其同事克隆出组胺H(3)受体cDNA以来，这种组胺受体已引起众多制药公司的关注，成为治疗包括肥胖症、注意力缺陷多动障碍、阿尔茨海默病、精神分裂症以及心肌缺血、偏头痛和炎症性疾病等各种重要疾病的潜在药物靶点。在此，我们讨论关于该靶蛋白的相关信息，并描述各种H(3)受体激动剂和拮抗剂的研发情况，以及它们在临床前动物模型中的作用。