Biological ActivityCTOP 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.
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X-5 = Orn, X-7 = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide)
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Intra-VTA injections of the mu-opioid antagonist CTOP enhance locomotor activity.
Badiani et al.
Brain Res., 1995;690:112
[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.
Hawkins et al.
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.
Gulya et al.
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
Chieng et al.
Citations for CTOP
The citations listed below are publications that use Tocris products. Selected citations for CTOP include:
12 Citations: Showing 1 - 10
Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
Authors: Nam Et al.
Cell Rep 2019;28:1154
A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action.
Authors: Stoeber Et al.
Selective blockade of spinal D2DR by levo-corydalmine attenuates MOR tolerance via suppressing PI3K/Akt-MAPK signaling in a MOR-dependent manner.
Authors: Dai Et al.
Exp Mol Med 2018;50:148
A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins.
Authors: Francois Et al.
Pronociceptive and Antinociceptive Effects of Bupren. in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.
Authors: Gerhold Et al.
J Neurosci 2015;35:9580
Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.
Authors: Morse Et al.
BMC Pharmacol Toxicol 2013;14:17
Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target.
Authors: Morse Et al.
PLoS One 2011;6:e25643
Activation of spinal mu- and δ-opioid receptors potently inhibits substance P release induced by peripheral noxious stimuli.
Authors: Beaudry Et al.
Mol Pharmacol 2011;31:13068
Evidence for a role of opioids in epoxyeicosatrienoic acid-induced cardioprotection in rat hearts.
Authors: Gross Et al.
Am J Physiol Heart Circ Physiol 2010;298:H2201
Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor.
Authors: Choi Et al.
Korean J Pain 2010;23:236
δ-opioid receptor expression in the ventral tegmental area protects against elevated alcohol consumption.
Authors: Margolis Et al.
J Clin Immunol 2008;28:12672
Cannabinoid receptor type 2 agonists induce transcription of the mu-opioid receptor gene in Jurkat T cells.
Authors: Börner Et al.
J Neurosci 2006;69:1486
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