1027330-97-7
1027330-97-7 structure
- Name: A-943931
- Chemical Name: 4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[1,2]cyclohepta[3,4-b]pyrimidin-2-amine
- CAS Number: 1027330-97-7
- Molecular Formula: C17H21N5
- Molecular Weight: 295.38200
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2017-06-23 20:53:59
- Modify Date: 2024-02-24 12:35:29
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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].
| Name | 4-[(3R)-3-aminopyrrolidin-1-yl]-6,7-dihydro-5H-benzo[1,2]cyclohepta[3,4-b]pyrimidin-2-amine |
|---|---|
| Synonyms |
2,4-diamino-5,6-disubstituted pyrimidine,10
UNII-Q598HK01AO |
| 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 |
| Molecular Formula | C17H21N5 |
|---|---|
| Molecular Weight | 295.38200 |
| Exact Mass | 295.18000 |
| PSA | 81.79000 |
| LogP | 2.44730 |