1152747-82-4
1152747-82-4 structure
- Name: Enerisant
- Chemical Name: enerisant
- CAS Number: 1152747-82-4
- Molecular Formula: C22H30N4O3
- Molecular Weight: 398.499
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2018-10-17 12:51:57
- Modify Date: 2024-01-14 20:31:42
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Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively[1].
| Name | enerisant |
|---|---|
| Synonyms |
E2Y97PQY3A
Methanone, [1-[4-[3-[(2R)-2-methyl-1-pyrrolidinyl]propoxy]phenyl]-1H-pyrazol-4-yl]-4-morpholinyl- 10095 enerisant [1-(4-{3-[(2R)-2-Methyl-1-pyrrolidinyl]propoxy}phenyl)-1H-pyrazol-4-yl](4-morpholinyl)methanone |
| Description | Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 2.89 nM (human histamine H3 receptor), 14.5 nM (rat histamine H3 receptor) Ki: 1.65 nM (human histamine H3 receptor), 7.87 nM (rat histamine H3 receptor)[1] |
| In Vivo | Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) 减弱大鼠的双食性反应[1]。 Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) 导致大鼠组胺 H3 受体以剂量依赖的方式被占用。引起半最大受体占用的剂量为 0.78 mg/kg[1]。 Enerisant hydrochloride (1 mg/kg; s.c.; once) 增加大鼠下丘脑后部的总细胞外组胺水平[1]。 Enerisant hydrochloride (1 mg/kg; i.p.; once) 增加大鼠内侧前额叶皮层 (mPFC) 的总细胞外多巴胺和乙酰胆碱水平[1]。 Animal Model: Male SD rats, R-α-methylhistamine-induced dipsogenia model[1] Dosage: 0.1, 0.3 and 1 mg/kg Administration: Oral, single dose Result: Attenuated the dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 586.2±50.0 °C at 760 mmHg |
| Molecular Formula | C22H30N4O3 |
| Molecular Weight | 398.499 |
| Flash Point | 308.3±30.1 °C |
| Exact Mass | 398.231781 |
| LogP | 1.49 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.620 |