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Irdabisant hydrochloride

CAS No. : 1005398-61-7

MCE 站：Irdabisant hydrochloride

产品活性：Irdabisant (CEP-26401) hydrochloride 是一种具有选择性、口服活性和血脑屏障渗透性的组胺 H3 受体 (histamine H3 receptor, H3R) 拮抗剂/逆激动剂，对大鼠 H3R 和人 H3R 的 K_i 分别为 7.2 nM 和 2.0 nM。Irdabisant hydrochloride 对 hERG 电流的抑制活性相对较低，IC₅₀ 为 13.8 μM。Irdabisant hydrochloride 在大鼠社会认知模型中具有认知增强和唤醒作用。Irdabisant hydrochloride 可用于精神分裂症或认知障碍的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Irdabisant (CEP-26401, compound 8a) shows antagonist activity with K_{b, app} values of 1.0 nM ａnd 0.4 nM for rat H3R ａnd human H3R, respectively; shows inverse agonist activity with EC₅₀ values of 2.0 nM ａnd 1.1 nM for rat H3R ａnd human H3R, respectively.
Irdabisant has moderate activity at Muscarinic M₂ (K_i = 3.7 ± 0.0 μM) ａnd Adrenergic α_1A (K_i = 9.8 ± 0.3 μM) receptors, Dopamine transporters (K_i = 11 ± 2 μM), Norepinephrine transporters (K_i = 10 ± 1 μM), ａnd phosphodiesterase PDE3 (IC₅₀ = 15 ± 1 μM).
Irdabisant inhibits the cytochrome P450 enzymes CYP1A2, 2C9, 2C19, 2D6, ａnd 3A4 with IC₅₀ values of greater than 30 μM, indicating less potential for drug-drug interactions.

In Vivo: CEP-26401 (0.01-0.3 mg/kg; p.o.; single dosage) dose-dependently inhibits H3R agonist RAMH-induced dipsogenia.
CEP-26401 (0.0001-0.1 mg/kg; i.v. or p.o.; single dosage) improves performance in the rat social recognition model of short-term memory.
CEP-26401 (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat.
CEP-26401 (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice.
CEP-26401 (1 mg/kg for i.v. ａnd 3 mg/kg for p.o.; single dosage) is rapidly absorbed with high oral bioavailability in rat ａnd monkey, ａnd shows a moderate clearance in monkey ａnd dog compared to the rat.
Pharmacokinetic Parameters of Irdabisant (compound 8a) in rats, dogs ａnd monkeys.

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