2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Irdabisant hydrochloride

Irdabisant hydrochloride  (Synonyms: CEP-26401 hydrochloride)

目录号: HY-109968A
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摩尔计算器

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 Ki 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。

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Irdabisant hydrochloride Chemical Structure

Irdabisant hydrochloride Chemical Structure

CAS No. : 1005398-61-7

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Irdabisant hydrochloride 的其他形式现货产品:

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Other Forms of Irdabisant hydrochloride:

Irdabisant hydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment[1][2].

IC50 & Target[1]

rat H3 receptor

7.2 nM (Ki)

human H3 receptor

2 nM (Ki)

体外研究
(In Vitro)

Irdabisant (CEP-26401, compound 8a) shows antagonist activity with Kb, 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[1].
Irdabisant has moderate activity at Muscarinic M2 (Ki = 3.7 ± 0.0 μM) and Adrenergic α1A (Ki = 9.8 ± 0.3 μM) receptors, Dopamine transporters (Ki = 11 ± 2 μM), Norepinephrine transporters (Ki = 10 ± 1 μM), and phosphodiesterase PDE3 (IC50 = 15 ± 1 μM)[1].
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[1].

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

Irdabisant hydrochloride 相关抗体:
体内研究
(In Vivo)

CEP-26401 (0.01-0.3 mg/kg; p.o.; single dosage) dose-dependently inhibits H3R agonist RAMH-induced dipsogenia[1].
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[1].
CEP-26401 (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat[2].
CEP-26401 (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice[2].
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[1].
Pharmacokinetic Parameters of Irdabisant (compound 8a) in rats, dogs and monkeys[1].

Rat Dog Monkey
i.v. t1/2 (h) 2.6 2.9 5.4
i.v. Vd (L/kg) 9.4 3.5 ± 1.1 3.8 ± 0.9
i.v. CL (mL/min/kg) 42 13.2 ± 1.5 7.7 ± 1.8
p.o. t1/2 (L/kg) 2.9 2.7 5.0
p.o. AUC (ng·h/mL) 984 1190 ± 180 1919 ± 611
p.o. Cmax (ng/mL) 270 230 ± 70 760 ± 74
p.o. F (%) 83 22 ± 2 83 ± 18
Brain to plasma ratio 2.6 ± 0.2 2.4 ± 0.4 /

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

Animal Model: Male Sprague-Dawley rats (i.p. 10 mg/kg RAMH-induced dipsogenia model)[1]
Dosage: 0.01-0.3 mg/kg
Administration: p.o.; single dosage
Result: Dose-dependently inhibited H3R agonist RAMH (HY-100999)-induced dipsogenia (which manifests as water drinking) with an EC50 value of 0.06 mg/kg.
Animal Model: Male Sprague-Dawley rats (adult rats were briefly exposed to a juvenile rat for build social recognition model)[2]
Dosage: 0.0001, 0.001, 0.01 and 0.1 mg/kg for i.p.; 0.01 and 0.1 mg/kg for p.o.
Administration: i.v. or p.o.; single dosage
Result: Effectively reduced the ratio of investigation duration (RID) at doses over the range from 0.001 to 0.1 mg/kg i.p. and at 0.01 and 0.1 mg/kg p.o., demonstrating potent enhancement of short-term sensory memory in this model.
Animal Model: Male Sprague-Dawley rats[2]
Dosage: 3, 10 and 30 mg/kg
Administration: p.o.; single dosage
Result: Exhibited robust wake promotion with the treated animals awake 90% of the time up to 3 h postdosing at 30 mg/kg.
Animal Model: Male Sprague-Dawley rats, male beagle dogs and male cynomolgus monkeys[1]
Dosage: 1 mg/kg for i.v. and 3 mg/kg for p.o.
Administration: i.v. and p.o.
Result: Exhibited rapid absorption with high oral bioavailability in rat and monkey, and showed a moderate clearance in monkey and dog compared to the rat.
Animal Model: Male DBA/2NCrl mice (19-27 g; 7-9 weeks)[2]
Dosage: 3, 10 and 30 mg/kg
Administration: i.p.; single dosage
Result: Increased prepulse inhibition (PPI) in DBA/2NCrl mice, whereas the antipsychotic Risperidone (HY-11018) is effective at 0.3 and 1 mg/kg i.p..
Clinical Trial
分子量

349.86

Formula

C18H24ClN3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Irdabisant hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Irdabisant1005398-61-7CEP-26401CEP26401CEP 26401Histamine Receptorblood-brain barrierhERGsocial recognition modelschizophreniaSD ratsDBA/2NCrl micebeagle dogscynomolgus monkeysInhibitorinhibitorinhibit

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