Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Bioorg Med Chem Lett
; 21(3): 1036-40, 2011 Feb 01.
Article
in En
| MEDLINE
| ID: mdl-21211969
ABSTRACT
Compound 21 (AM432) was identified as a potent and selective antagonist of the DP(2) receptor (CRTH2). Modification of a bi-aryl core identified a series of tri-aryl antagonists of which compound 21 proved a viable clinical candidate. AM432 shows excellent potency in a human whole blood eosinophil shape change assay with prolonged incubation, a comparatively long off-rate from the DP(2) receptor, excellent pharmacokinetics in dog and in vivo activity in two mouse models of inflammatory disease after oral dosing.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Phenylacetates
/
Pyridines
/
Receptors, Prostaglandin
/
Receptors, Immunologic
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2011
Type:
Article
Affiliation country:
United States