Potent and selective NOP receptor antagonist (IC50 values are 0.27, 2500, 6700 and > 10000nM 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.
Chemical Name: (2R)-1-(Phenylmethyl)-N-[3-(spiro[isobenzofuran-1(3H),4'-piperidin]-1-yl)propyl-2-pyrrolidinecarboxamide
CAS Number: 1401463-54-4
Solubility: Soluble to 100mM in water and to 100mM in DMSO
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