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)
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solubility||Soluble to 1 mg/ml in water|
References are publications that support the biological activity of the product.
Calo et al (2002) [Nphe1,Arg14,Lys15]Nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. Br.J.Pharmacol. 136 303 PMID: 12010780
Gavioli et al (2003) Blockade of nociceptin/orphanin FQ-NOP receptor signalling produces antidepressant-like effects: pharmacological and genetic evidences from the mouse forced swimming test. Eur.J.Neurosci. 17 1987 PMID: 12752799
Marti et al (2003) Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex. Br.J.Pharmacol. 138 91 PMID: 12522077
McDonald et al (2003) UFP-101, a high affinity antagonist for the nociceptin/orphanin FQ receptor: radioligand and GTPγ35 binding studies. Naunyn Schmiedebergs Arch.Pharmacol. 367 183 PMID: 12595960
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Keywords: UFP-101, UFP-101 supplier, Potent, selective, silent, antagonists, NOP, Nociceptin, Receptors, ORL1, OP4, Opioid, [Nphe1,Arg14,Lys15]Nociceptin-NH2, 1552, Tocris Bioscience
2 Citations for UFP-101
Citations are publications that use Tocris products. Selected citations for UFP-101 include:
Mahmoud et al (2010) Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol 77 804 PMID: 20159949
Kuzmin et al (2004) Evidence in locomotion test for the functional heterogeneity of ORL-1 receptors. Br J Pharmacol 141 132 PMID: 14662736
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.