Aticaprant (CERC-501) 是一种有效地可渗透中枢神经的kappa opioid受体拮抗剂，K_i值为0.807 nM。

Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K i of 0.807 nM.

Solid

Ki: 0.807 nM (kappa opioid)

Aticaprant (CERC-501) binds with high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu opioid receptor and 190-fold higher affinity over the human delta opioid receptor. Aticaprant (CERC-501) shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors or ion channel/transporter binding targets or the central benzodiazepine binding site. has not independently confirmed the accuracy of these methods. They are for reference only.

Aticaprant (CERC-501) has a rapid absorption (t max =1-2 h) and good oral bioavailability (F=25%). Oral Aticaprant (CERC-501) administration selectively and potently occupies central kappa opioid receptors (ED 50 =0.33 mg/kg), 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 (CERC-501) produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. Aticaprant (CERC-501) reduces ethanol self-administration in alcohol-preferring rats. Aticaprant (CERC-501) alleviates the nicotine withdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal induced anxiety-related behavior, somatic signs, and CPA, and

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Rorick-Kehn LM, 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.
[2]. Jackson KJ, et al. Effects of orally-bioavailable short-acting kappa opioid receptor-selective antagonist LY2456302on nicotine withdrawal in mice. Neuropharmacology. 2015 Oct;97:270-4.

In Vitro: DMSO : ≥ 100 mg/mL (238.95 mM)配制储备液