CTOP

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Cat.No. 1578 - CTOP | D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (Disulfide bridge: 2 - 7) | CAS No. 103429-31-8
Description: Potent and selective μ antagonist
Datasheet
Citations (8)
Reviews
Literature

Biological Activity

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

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 between 2 - 7, Thr-8 = C-terminal amide)

Storage Desiccate at -20°C
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solubility Soluble to 1 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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Keywords: CTOP, CTOP supplier, selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Mu, Opioid, 1578, Tocris Bioscience

8 Citations for CTOP

Citations are publications that use Tocris products. Selected citations for CTOP include:

Gerhold et al (2015) Pronociceptive and Antinociceptive Effects of Buprenorphine 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

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

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

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

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 (2011) Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target. PLoS One 6 e25643 PMID: 22003401


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