| Identification | Back Directory | [Name]
Enerisant | [CAS]
1152747-82-4 | [Synonyms]
Enerisant
Methanone, [1-[4-[3-[(2R)-2-methyl-1-pyrrolidinyl]propoxy]phenyl]-1H-pyrazol-4-yl]-4-morpholinyl- | [Molecular Formula]
C22H30N4O3 | [MOL File]
1152747-82-4.mol | [Molecular Weight]
398.5 |
| Hazard Information | Back Directory | [Uses]
Enerisant (TS-091) 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]. | [in vivo]
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]. | 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. |
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