同义名 :	CERC-501; Ly2456302; JNJ-67953964; LY-2456302
	CAS号 :	1174130-61-0
	货号 :	A354780
	分子式 :	C26H27FN2O2
	纯度 :	99%+
	分子量 :	418.5
	MDL号 :	MFCD22572355
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

Aticaprant, also known as CERC-501, binds to the human kappa opioid receptor with high affinity, having a Ki value of 0.807 nM. Its affinity is 30 times greater for the human mu opioid receptor and 190 times greater for the human delta opioid receptor. Aticaprant shows no significant affinity for several non-opioid cell surface G-protein coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors, or ion channel/transport protein binding targets or the central benzodiazepine binding site[1].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.39mL 0.48mL 0.24mL	11.95mL 2.39mL 1.19mL	23.89mL 4.78mL 2.39mL

参考文献

[1]Lowe SL, Wong CJ, Witcher J, et al. Safety, tolerability, and pharmacokinetic evaluation of single- and multiple-ascending doses of a novel kappa opioid receptor antagonist LY2456302 and drug interaction with ethanol in healthy subjects. J Clin Pharmacol. 2014 Sep;54(9):968-78. [2]Rorick-Kehn LM, Witkin JM, et al. LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44.