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Submit ReviewUFP-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.
分子量 | 1908.19 |
公式 | C82H138N32O21 |
序列 |
GGGFTGARKSARKRKNQ (Modifications: Gly-1 = N-(Bn)Gly, Gln-17 = C-terminal amide) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 849024-68-6 |
PubChem ID | 16152632 |
InChI Key | DOLKPWDXAQZKNJ-LGCGZHPXSA-N |
Smiles | C[C@@H](O)[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)CNCC1=CC=CC=C1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: UFP-101, UFP-101 supplier, Potent, selective, silent, antagonists, NOP, Nociceptin, Receptors, ORL1, OP4, Opioid, [Nphe1,Arg14,Lys15]Nociceptin-NH2, 1552, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 UFP-101 的部分引用包括:
Wang et al (2019) Nociceptin Receptor Is Overexpressed in Non-small Cell Lung Cancer and Predicts Poor Prognosis. Front Oncol 9 235 PMID: 31024840
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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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.