Potent, selective and competitive silent antagonist for the NOP opioid receptor. Binds to NOP with high affinity (pKi
= 10.24) and displays > 3000-fold selectivity over δ
opioid receptors. Antinociceptive and opposes the action of nociceptin in vivo
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[Nphe1,Arg14,Lys15]Nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.
Calo et al.
Blockade of nociceptin/orphanin FQ-NOP receptor signalling produces antidepressant-like effects: pharmacological and genetic evidences from the mouse forced swimming test.
Gavioli et al.
UFP-101, a high affinity antagonist for the nociceptin/orphanin FQ receptor: radioligand and GTPγ35 binding studies.
McDonald et al.
Naunyn Schmiedebergs Arch.Pharmacol., 2003;367:183
Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex.
Marti et al.
The citations listed below are publications that use Tocris products. Selected citations for UFP-101 include:
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