Enerisant

Names

[ Name ]:
Enerisant

[Synonym ]:
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

Biological Activity

[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]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

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

[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]

[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.

Chemical & Physical Properties

[ 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

Related Compounds

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