A-943931
Names
[ CAS No. ]:
1027330-97-7
[ 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]:
[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]
Chemical & Physical Properties
[ Molecular Formula ]:
C17H21N5
[ Molecular Weight ]:
295.38200
[ Exact Mass ]:
295.18000
[ PSA ]:
81.79000
[ LogP ]:
2.44730