| 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 |
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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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