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Description: BAN ORL 24 is a novel, potent and selective NOP (nociceptin/orphanin FQ (N/OFQ) peptide receptor) receptor antagonist with IC50 values of 0.27, 2500, 6700 and > 10000 nM for NOP, kappa-, u- and delta-receptors respectively. NOP receptor mediates anti-analgesia induced by agonist-antagonist opioids. Compound 24 (BAN ORL 24) up to 1 microM did not modify the effects of classical opioid receptor agonists. Finally in vivo, in the mouse tail withdrawal assay, Compound 24 at 10 mg/kg antagonized the pronociceptive and antinociceptive effects of 1 nmol N/OFQ given supraspinally and spinally, respectively. Under the same experimental conditions Compound 24 did not affect the antinociceptive action of 3 nmol endomorphin-1 injected intrathecally. The present study demonstrated that Compound 24 is a pure, competitive, and highly potent non-peptide NOP receptor selective antagonist.
References: Eur J Pharmacol. 2009 Jul 1; 614(1-3):50-7.
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