MCOPPB (hydrochloride hydrate)|安捷凯

Background

The nociceptin/orphanin FQ peptide (NOP, ORL1, or OP4) receptor is a member of the opioid family of receptors that integrates the emotional components of anxiety, fear, and stress. MCOPPB is a potent agonist for the NOP receptor (pK_i = 10.1, EC₅₀ = 0.39 nM) with 12-, 270-, and >1,000-fold selectivity over the μ-, κ-, and δ-opioid receptors.^1,2 In rodents, MCOPPB at 10 mg/kg, p.o. produces potent anxiolytic effects, without inhibiting memory or motor function or inducing sedative side effects.¹ This product is intended for research purposes only.

1.Hirao, A., Imai, A., Sugie, Y., et al.Pharmacological characterization of the newly synthesized nociceptin/orphanin FQ-receptor agonist 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole as an anxiolytic agentJournal of Pharmacological Sciences106361-368(2008) 2.Hayashi, S., Hirao, A., Imai, A., et al.Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: Design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drugJournal of Medicinal Chemistry52610-625(2009)

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MCOPPB (hydrochloride hydrate)

MCOPPB (hydrochloride hydrate)详情

Background

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