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1027330-97-7

1027330-97-7 Structure

1027330-97-7 Structure
IdentificationBack Directory
[Name]

A-943931
[CAS]

1027330-97-7
[Synonyms]

A-943931
4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-amine
5H-Benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-amine, 4-[(3R)-3-amino-1-pyrrolidinyl]-6,7-dihydro-
[Molecular Formula]

C17H21N5
[MOL File]

1027330-97-7.mol
[Molecular Weight]

295.38
Hazard InformationBack Directory
[Uses]

A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy[1][2].
[in vivo]

A-943931 shows anti-inflammatory activity in zymosan-induced peritonitis in mice with the ED50s of 34, 33 μmol/kg for s.c. and i.p., respectively[2].
A-943931 (10, 30, 100 μmol/kg; i.p.) shows antinociceptive efficacy in inflammatory pain and neuropathic pain model in rats[2].

Animal Model:Rats (carrageenan-induced inflammatory pain and spinal nerve ligation model of neuropathic pain)[2]
Dosage:10, 30, 100 μmol/kg
Administration:I.p.
Result:Showed antinociceptive efficacy in an inflammatory pain model in rat at an ED50 value of 72 μmol/kg, ip, and in a neuropathic pain model at an ED50 value of 100 μmol/kg, ip.
[IC 50]

Human H4 Receptor: 4.6 nM (Ki); Rat H4 receptor: 3.8 nM (Ki)
[References]

[1] Ivan Milicic, et al. Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activity. The FASEB journal homepage. 2009.
[2] Cowart MD, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem. 2008 Oct 23;51(20):6547-57. DOI:10.1021/jm800670r
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