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.
(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|
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||Soluble to 1 mg/ml in water|
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
8 Citations for CTOP
Citations are publications that use Tocris products. Selected citations for CTOP include:
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
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
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
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
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
Do you know of a great paper that uses CTOP from Tocris? Please let us know.
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
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.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
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