Molecular and biochemical pharmacology of the histamine H4 receptor
نویسندگان
چکیده
منابع مشابه
Molecular modeling and site-specific mutagenesis of the histamine-binding site of the histamine H4 receptor.
The histamine H4 receptor is a novel G-protein-coupled receptor with a unique pharmacological profile. The distribution of H4 mRNA suggests that it may play a role in the regulation of immune function, particularly with respect to allergy and asthma. To define the histamine-binding site of this receptor, molecular modeling and site-directed mutagenesis were used to predict and alter amino acids...
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Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist with a Ki at the human receptor of 8.4 ± 2.2 nM and excellent selectivity over other receptors including the other histamine receptors. The compound acts as an antagonist in all species tested and inhibits histamine-induced eosinophil shape change in vitro. Toreforant was anti-inflammatory in mouse models of asthma and ...
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The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H(1)R ligands bind to hH(4)R. In an acute murine asthma model, the H(1)R antago...
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Since 2000, when the histamine H4 receptor (H4R) was cloned, it has constituted an interesting target for drug development. Pharmacological studies suggest the potential utility of histamine H4R antagonists/inverse agonists in the treatment of inflammatory diseases, e.g. allergic rhinitis, asthma, atopic dermatitis, colitis, or pruritus. The first H4R ligands were non-selective compounds, but i...
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Correspondence: Robin L Thurmond Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, UsA email [email protected] Abstract: The histamine H 4 receptor (H 4 R) has generated excitement as a potential target for the development of novel anti-inflammatory therapies. However, many of its physiological functions are still being uncovered and...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2009
ISSN: 0007-1188,1476-5381
DOI: 10.1111/j.1476-5381.2009.00250.x