Identification | Back 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 Information | Back 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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BOC Sciences
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https://www.bocsci.com |
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