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 (4)
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

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 1062.28. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.94 mL 4.71 mL 9.41 mL
5 mM 0.19 mL 0.94 mL 1.88 mL
10 mM 0.09 mL 0.47 mL 0.94 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

4 Citations for CTOP

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

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

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

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

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


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