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Drug Discov Today. 2009 May;14(9-10):509-15. doi: 10.1016/j.drudis.2009.02.011. Epub 2009 Mar 6.

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

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1
Evotec AG, Schnackenburgallee 114, 22525 Hamburg, Germany. mark.gemkow@evotec.com

Abstract

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.

PMID:
19429511
DOI:
10.1016/j.drudis.2009.02.011
[Indexed for MEDLINE]
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