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Aticaprant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aticaprant图片
CAS NO:1174130-61-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
LY-2456302
CERC-501
产品介绍
Aticaprant 是一种有效的中枢渗透性 kappa-阿片受体拮抗剂,Ki值为 0.807 nM。

产品描述

Aticaprant (CERC-501) is a potent and centrally-penetrant antagonist of the kappa-opioid receptor (Ki: 0.807 nM).

体外活性

Aticaprant binds with a high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu-opioid receptor and a 190-fold higher affinity over the human delta-opioid receptor. Aticaprant shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets [1].

体内活性

Aticaprant has rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Aticaprant selectively and potently occupies central kappa opioid receptors (ED50: 0.33 mg/kg, p.o.), without evidence of mu or delta receptor occupancy. LY2456302 potently blocks kappa-agonist-mediated analgesia and disruption of prepulse inhibition, without affecting mu-agonist-mediated effects at doses >30-fold higher. Aticaprant produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. Aticaprant reduces ethanol self-administration in alcohol-preferring rats [1]. Aticaprant alleviates the nicotine withdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal-induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment [2].

动物实验

Three male cannulated rats are administered a single 1 mg/kg intravenous (IV) and 10 mg/kg oral (PO) dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.08 (IV only), 0.25, 0.5, 1, 2, 4, 8, 12 and 24 h post-dose and analyzed by liquid chromatography coupled to tandem mass spectral detection to determine the concentrations of Aticaprant (CERC-501). Male mice are administered a single 10 mg/kg PO dose of Aticaprant to determine the pharmacokinetic parameters. Plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h post-dose and analyzed by LCMS/MS to determine the concentrations of Aticaprant. The plasma and brain binding of Aticaprant is determined by equilibrium dialysis at 1 μM [1].

Cas No.

1174130-61-0

分子式

C26H27FN2O2

分子量

418.5

别名

LY-2456302;CERC-501

储存和溶解度

DMSO:100 mg/mL (238.95 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years