Document Detail

Histamine H4 receptor ligands and their potential therapeutic applications: an update.
MedLine Citation:
PMID:  22385042     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Several studies underlined the critical role of histamine H4 receptor (H4R) in inflammation, thus H4 modulators have been suggested as promising drug candidates in inflammatory diseases. First H4 ligands typically have indole or amino-pyrimidine scaffolds. During the last few years, however, serious efforts have been made to identify novel H4 chemotypes with improved pharmacodynamic and pharmacokinetic properties.
AREAS COVERED: Areas covered in this review include an overview on H4 ligands published in scientific papers, as well as in patent applications between 2009 and 2011. Recently discovered scaffolds possessing significant H4 activity were analyzed and their therapeutic potential was reviewed.
EXPERT OPINION: Recent results from the scientific literature and novel patent applications reinforce the major role of H4R in inflammatory diseases such as pruritus, asthma, inflammatory pain and allergic rhinitis. Novel studies suggest further indications of H4 modulators in cancer, neuropathic pain, vestibular disorders and type 2 diabetes. The number of active H4 chemotypes was increased significantly. The first H4 antagonist entered to clinics and the results from a proof-of-concept Phase II clinical study is expected to be disclosed soon.
Róbert Kiss; György M Keserű
Publication Detail:
Type:  Journal Article; Review     Date:  2012-03-03
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Mar 
Date Detail:
Created Date:  2012-03-14     Completed Date:  2012-07-03     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  205-21     Citation Subset:  IM    
Affiliation: Ltd., Vendel u. 15-17, H-1096, Budapest, Hungary.
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MeSH Terms
Anti-Inflammatory Agents / chemistry,  pharmacokinetics,  pharmacology
Drug Design
Histamine Antagonists / chemistry,  pharmacokinetics,  pharmacology*
Inflammation / drug therapy*,  physiopathology
Patents as Topic
Receptors, G-Protein-Coupled / drug effects*,  metabolism
Receptors, Histamine / drug effects*,  metabolism
Reg. No./Substance:
0/Anti-Inflammatory Agents; 0/HRH4 protein, human; 0/Histamine Antagonists; 0/Ligands; 0/Receptors, G-Protein-Coupled; 0/Receptors, Histamine

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