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Aticaprant

CAS No. : 1174130-61-0

產(chǎn)品活性：Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K_i of 0.807 nM.

研究領(lǐng)域：GPCR/G Protein  |  Neuronal Signaling

作用靶點(diǎn)：Opioid Receptor

In Vitro: 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.

In Vivo: 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 (ED₅₀=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withdrawal induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment.

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