BAN ORL 24

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Product Code: 6817
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Chemical Name: (2R)-1-(Phenylmethyl)-N-[3-(spiro[isobenzofuran-1(3H),4'-piperidin]-1-yl)propyl-2-pyrrolidinecarboxamide

Biological Activity:
Biological Activity	Potent and selective NOP receptor antagonist (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively). Inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro and antagonizes NOP agonist-induced reduction in locomotor activity in vivo. Brain penetrant.
Technical Data:
M.W.	506.51
Formula:	C<sub>27</sub>H<sub>35</sub>N<sub>3</sub>O<sub>2</sub>.2HCl
Solubility:	Soluble to 100 mM in water and to 100 mM in DMSO
CAS No:	1401463-54-4
References:
References	Goto et al (2006) Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity. J.Med.Chem. 49 847. PMID: 16451050. Fischetti et al (2009) Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist compound 24. Eur.J.Pharmacol. 614 50. PMID: 19445927. Liao et al (2009) 1-Benzyl-N-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl]pyrrolidine-2-carboxamide (compound 24) antagonizes NOP receptor-mediated potassium channel activation in rat periaqueductal gray slices. Eur.J.Pharmacol. 606 84. PMID: 19374842.

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