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Description: Potent and selective μ antagonist
Purity: ≥95% (HPLC)
Biological Activity 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.
Technical Data for CTOP
| M. Wt | 1062.28 |
| Formula | C50H67N11O11S2 |
| Sequence |
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) |
| Storage | Store at -20°C |
| Purity | ≥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 |
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 Data for CTOP
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for CTOP
References for CTOP
References are publications that support the biological activity of the product.
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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Keywords: CTOP, CTOP supplier, selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, 1578, Tocris Bioscience
12 Citations for CTOP
Citations are publications that use Tocris products. Selected citations for CTOP include:
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
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
Stoeber et al (2018) A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action. Neuron 98 963 PMID: 29754753
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
Francois et al (2017) A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins. Neuron 93 822 PMID: 28162807
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
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
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
Nam et al (2019) Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference. Cell Rep 28 1154 PMID: 31365861
Do you know of a great paper that uses CTOP from Tocris? Please let us know.
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