Aticaprant Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

418.5

DMSO: 100mg/mL (238.95mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C26H27FN2O2

Cc1cc([C@H]2N(Cc(cc3)ccc3Oc(ccc(C(N)=O)c3)c3F)CCC2)cc(C)c1

1174130-61-0

Aticaprant has rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Aticaprant selectively and potently occupies central kappa opioid receptors (ED50: 0.33mg/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withdrawal-induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment,[2].

Endocrinology/Hormones; Opioid Receptor