A-943931

Names

[ Name ]:
A-943931

[Synonym ]:
2,4-diamino-5,6-disubstituted pyrimidine,10
UNII-Q598HK01AO

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

Human H4 Receptor:4.6 nM (Ki)

Rat H4 receptor:3.8 nM (Ki)

[In Vivo]

A-943931 在酵母聚糖诱导的小鼠腹膜炎中表现出抗炎活性，皮下注射和腹腔注射的ED50 值分别为 34, 33 µmol/kg[2]。 A-943931 (10, 30, 100 µmol/kg; 腹腔注射) 在大鼠的炎症性疼痛和神经性疼痛模型中表现出镇痛效果[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₂₁N₅

[ Molecular Weight ]:
295.38200

[ Exact Mass ]:
295.18000

[ PSA ]:
81.79000

[ LogP ]:
2.44730

Related Compounds

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