The histamine H3 receptor as a therapeutic drug target for CNS disorders

被引：155

作者：

Gemkow, Mark J. ^{[1
]}

Davenport, Adam J. ^{[2
]}

Harich, Silke ^{[1
]}

Ellenbroek, Bart A. ^{[1
]}

Cesura, Andrea ^{[1
]}

Hallett, David ^{[2
]}

机构：

[1] Evotec AG, D-22525 Hamburg, Germany

[2] Evotec UK Ltd, Abingdon OX14 4SA, Oxon, England

来源：

DRUG DISCOVERY TODAY | 2009年 / 14卷 / 9-10期

关键词：

RAT-BRAIN CORTEX; H-3; RECEPTOR; ANTAGONISTS/INVERSE AGONISTS; PRECLINICAL PHARMACOLOGY; COGNITIVE DISORDERS; INVERSE AGONISTS; INHIBITION; RELEASE; POTENT; H-3-RECEPTOR;

D O I：

10.1016/j.drudis.2009.02.011

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The histamine H3 receptor plays a regulatory role in the pre-synaptic release of histamine and other neurotransmitters, making it an attractive target for CNS indications including cognitive disorders, narcolepsy, ADHD and pain. As more and more H3 antagonists/H3 inverse agonists progress through the clinic, knowledge is gained to define the profile of the 'ideal' compound in terms of specificity, pharmacokinetic parameters and both duration and magnitude of receptor occupancy. Whether a single compound profile for the treatment of different disorders can be defined remains to be seen.

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收藏

页码：509 / 515

页数：7

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