Enerisant_product_DataBase

Bioactivity	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].
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)
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:
Name	Enerisant
CAS	1152747-82-4
Formula	C22H30N4O3
Molar Mass	398.50
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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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