Introduction：Basic information about CAS 1152747-82-4|Enerisant, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Enerisant |
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| CAS Number | 1152747-82-4 | Molecular Weight | 398.499 |
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| Density | 1.2±0.1 g/cm3 | Boiling Point | 586.2±50.0 °C at 760 mmHg |
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| Molecular Formula | C22H30N4O3 | Melting Point | / |
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| MSDS | / | Flash Point | 308.3±30.1 °C |
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Names
| Name | enerisant |
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| Synonym | More Synonyms |
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Enerisant BiologicalActivity
| 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]. |
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| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>Histamine Receptor |
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| 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] |
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| 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. |
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| References | [1]. Hino N, et al. A novel potent and selective histamine H3 receptor antagonist enerisant: in vitro profiles, in vivo receptor occupancy, and wake-promoting and procognitive effects in rodents. Journal of Pharmacology and Experimental Therapeutics, 2020, 375(2): 276-285. |
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Chemical & Physical Properties
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 586.2±50.0 °C at 760 mmHg |
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| Molecular Formula | C22H30N4O3 |
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| Molecular Weight | 398.499 |
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| Flash Point | 308.3±30.1 °C |
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| Exact Mass | 398.231781 |
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| LogP | 1.49 |
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| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
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| Index of Refraction | 1.620 |
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| InChIKey | IABXVJILZYNSTM-GOSISDBHSA-N |
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| SMILES | CC1CCCN1CCCOc1ccc(-n2cc(C(=O)N3CCOCC3)cn2)cc1 |
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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 |
