Potent and selective nociceptin opioid receptor (NOP) agonist (EC50
values are 12, 693, 683 and 8071 nM, and Ki
values are 0.3, 65, 131 and 2854 nM at NOP, μ
- and δ
-opioid receptors respectively). Exhibits anxiolytic-like activity at doses that have no effect on overt behaviors such as locomotion in vivo
. Orally active.
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All Tocris products are intended for laboratory research use only.
The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510).
Varty et al.
The nociceptin/orphanin FQ receptor: a target with broad therapeutic potential.
Nat.Rev.Drug Discov., 2008;7:694
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
Yang et al.