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Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils.

Abstract:

D prostanoid receptor 2 (DP₂) [also known as chemoattractant receptor-homologous molecule expressed on T helper 2 (Th2) cells (CRTH2)] is selectively expressed by Th2 lymphocytes, eosinophils, and basophils and mediates recruitment and activation of these cell types in response to prostaglandin D₂ (PGD₂). (5-Fluoro-2-methyl-3-quinolin-2-ylmethylindo-1-yl)-acetic acid (OC000459) is an indole-acetic acid derivative that potently displaces [³H]PGD₂ from human recombinant DP₂ (K(i) = 0.013 μM), r...

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Publisher copy:
10.1124/jpet.111.187203

Authors


Pettipher, R More by this author
Vinall, SL More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Experimental Medicine Division,
Speight, G More by this author
Townsend, ER More by this author
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Journal:
The Journal of pharmacology and experimental therapeutics
Volume:
340
Issue:
2
Pages:
473-482
Publication date:
2012-02-05
DOI:
EISSN:
1521-0103
ISSN:
0022-3565
URN:
uuid:f082c43e-af94-4841-8bd5-c85969c61744
Source identifiers:
206047
Local pid:
pubs:206047

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