Enerisant 

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].

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]

Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) attenuats the dipsogenia response in rats^[1].
Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) results in the occupancy of the histamine H₃ receptor in a dose-dependent manner in rats. A dose eliciting a half-maximal receptor occupancy is 0.78 mg/kg^[1].
Enerisant hydrochloride (1 mg/kg; s.c.; once) increases the total extracellular histamine levels in the posterior hypothalamus in rats^[1].
Enerisant hydrochloride (1 mg/kg; i.p.; once) increases the total extracellular dopamine and acetylcholine levels in the medial prefrontal cortex (mPFC) in rats^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

398.50

C₂₂H₃₀N₄O₃

1152747-82-4

O=C(C1=CN(C2=CC=C(OCCCN3[[email protected]](C)CCC3)C=C2)N=C1)N4CCOCC4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.