CTOP
Purity: ≥95%
Biological Activity
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
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X-5 = Orn, X-7 = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide)
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.
Background References
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Opioid receptor-dependent sex differences in synaptic plasticity in the hippocampal mossy fiber pathway of the adult rat.
Harte-Hargrove L, Varga-Wesson A, Duffy A, Milner T, Scharfman H
J Neurosci, 2015;35(4):1723-38. -
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.
J.Pharmacol.Exp.Ther., 1989;248:73 -
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.
Eur.J.Pharmacol., 1988;150:355 -
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.
Mol.Pharmacol., 1996;50:650
Product Datasheets
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Citations for CTOP
The citations listed below are publications that use Tocris products. Selected citations for CTOP include:
12 Citations: Showing 1 - 10
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Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
Authors: Nam Et al.
Cell Rep 2019;28:1154
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A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action.
Authors: Stoeber Et al.
Neuron 2018;98:963
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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
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A Brainstem-Spinal Cord Inhibitory Circuit for Mechanical Pain Modulation by GABA and Enkephalins.
Authors: Francois Et al.
Neuron 2017;93:822
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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
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Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.
Authors: Morse Et al.
BMC Pharmacol Toxicol 2013;14:17
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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
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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
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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
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Roles of opioid receptor subtype in the spinal antinociception of selective cyclooxygenase 2 inhibitor.
Authors: Choi Et al.
Korean J Pain 2010;23:236
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δ-opioid receptor expression in the ventral tegmental area protects against elevated alcohol consumption.
Authors: Margolis Et al.
J Clin Immunol 2008;28:12672
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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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