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Submit ReviewCTOP
说明： Potent and selective μ antagonist
纯度： ≥95% (HPLC)
生物活性 for CTOP
CTOP is a potent and selective μ opioid receptor antagonist (Ki values are 0.96 and >10,000 nM for μ and δ receptors respectively). Causes behavioral effects on central administration in vivo. Also increases K+ currents in rat locus ceruleus neurons in vitro via a μ receptor independent mechanism.
技术数据 for CTOP
| 分子量 | 1062.28 |
| 公式 | C50H67N11O11S2 |
| 序列 |
FCYWXTXT (Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X-5 = Orn, X-7 = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 103429-31-8 |
| PubChem ID | 90479805 |
| InChI Key | PZWWYAHWHHNCHO-KOFBULAQSA-N |
| Smiles | [H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@H]1CSSC(C)(C)C(NC(=O)[C@@H](NC(=O)[C@H](CCCN)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC1=O)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)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.
溶解性数据 for CTOP
| 溶解性 | Soluble to 1 mg/ml in water |
产品说明书 for CTOP
参考文献 for CTOP
参考文献是支持产品生物活性的出版物。
Badiani et al (1995) Intra-VTA injections of the mu-opioid antagonist CTOP enhance locomotor activity. Brain Res. 690 112 PMID: 7496796
Gulya et al (1988) Central effects of the potent and highly selective mu opioid antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) in mice. Eur.J.Pharmacol. 150 355 PMID: 2901358
Hawkins et al (1989) [3H]-[H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2] ([3H]CTOP), a potent and highly selective peptide for mu opioid receptors in rat brain. J.Pharmacol.Exp.Ther. 248 73 PMID: 2563293
Chieng et al (1996) The μ-opioid receptor antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) [but not D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP)] produces a no Mol.Pharmacol. 50 650 PMID: 8794906
If you know of a relevant reference for CTOP, please let us know.
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关键词: CTOP, CTOP supplier, selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, 1578, Tocris Bioscience
12 篇 CTOP 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CTOP 的部分引用包括：
Beaudry et al (2011) Activation of spinal mu- and δ-opioid receptors potently inhibits substance P release induced by peripheral noxious stimuli. Mol Pharmacol 31 13068 PMID: 21917790
Francois et al (2017) A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins. Neuron 93 822 PMID: 28162807
Nam et al (2019) Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference. Cell Rep 28 1154 PMID: 31365861
Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci 35 9580 PMID: 26134641
Margolis et al (2008) δ-opioid receptor expression in the ventral tegmental area protects against elevated alcohol consumption. J Clin Immunol 28 12672 PMID: 19036960
Stoeber et al (2018) A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action. Neuron 98 963 PMID: 29754753
Morse et al (2011) Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target. PLoS One 6 e25643 PMID: 22003401
Dai et al (2018) Selective blockade of spinal D2DR by levo-corydalmine attenuates MOR tolerance via suppressing PI3K/Akt-MAPK signaling in a MOR-dependent manner. Exp Mol Med 50 148 PMID: 30429454
Choi et al (2010) Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor. Korean J Pain 23 236 PMID: 21217886
Gross et al (2010) Evidence for a role of opioids in epoxyeicosatrienoic acid-induced cardioprotection in rat hearts. Am J Physiol Heart Circ Physiol 298 H2201 PMID: 20400686
Morse et al (2013) Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family. BMC Pharmacol Toxicol 14 17 PMID: 23497702
Börner et al (2006) Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells. J Neurosci 69 1486 PMID: 16434616
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