Biological ActivityUFP-101 is a 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, μ and κ opioid receptors. Antinociceptive and opposes the action of nociceptin in vivo.
(Modifications: Gly-1 = N-(Bn)Gly, Gln-17 = C-terminal amide)
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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.
[Nphe1,Arg14,Lys15]Nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.
Calo 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.
Citations for UFP-101
The citations listed below are publications that use Tocris products. Selected citations for UFP-101 include:
3 Citations: Showing 1 - 3
Nociceptin Receptor Is Overexpressed in Non-small Cell Lung Cancer and Predicts Poor Prognosis.
Authors: Wang Et al.
Front Oncol 2019;9:235
Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons.
Authors: Mahmoud Et al.
Mol Pharmacol 2010;77:804
Evidence in locomotion test for the functional heterogeneity of ORL-1 receptors.
Authors: Kuzmin Et al.
Br J Pharmacol 2004;141:132
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