Biological ActivityCTAP is a potent and selective μ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over δ opioid and somatostatin receptors. Brain penetrant and active in vivo.
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge: 2-7, Thr-8 = C-terminal amide)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo.
Kramer et al.
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors.
Pelton et al.
Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with mor.
Abbruscato et al.
Citations for CTAP
The citations listed below are publications that use Tocris products. Selected citations for CTAP include:
13 Citations: Showing 1 - 10
Synapse-specific opioid modulation of thalamo-cortico-striatal circuits.
Authors: Birdsong Et al.
MOR-Induced Modulation of Endolysosomal Iron Mediates Upregulation of Ferritin Heavy Chain in Cortical Neurons.
Authors: Nash Et al.
Differential Desensitization Observed at Multiple Effectors of Somatic μ-Opioid Receptors Underlies Sustained Agonist-Mediated Inhibition of Proopiomelanocortin Neuron Activity.
Authors: Fox and Hentges
J Neurosci 2017;37:8667
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
Anti-analgesic effect of the mu/delta opioid receptor heteromer revealed by ligand-biased antagonism.
Authors: Milan-Lobo Et al.
PLoS One 2013;8:e58362
Building a better analgesic: multifunctional compounds that address injury-induced pathology to enhance analgesic efficacy while eliminating unwanted side effects.
Authors: Largent-Milnes Et al.
J Pharmacol Exp Ther 2013;347:7
Differences in the characteristics of tolerance to μ-opioid receptor agonists in the colon from wild type and β-arrestin2 knockout mice.
Authors: Maguma Et al.
Eur J Pharmacol 2012;685:133
Multiple inhibitory G-protein-coupled receptors resist acute desensitization in the presynaptic but not postsynaptic compartments of neurons.
Authors: Pennock Et al.
J Neurosci 2012;32:10192
Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation.
Authors: Krook-Magnuson Et al.
J Neurosci 2011;31:14861
Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5.
Authors: Song Et al.
J Biol Chem 2011;286:20354
Morphine increases brain levels of ferritin heavy chain leading to inhibition of CXCR4-mediated survival signaling in neurons.
Authors: Sengupta Et al.
J Leukoc Biol 2009;29:2534
DAMGO-induced expression of chemokines and chemokine receptors: the role of TGF-β1.
Authors: Happel Et al.
Front Cell Neurosci 2008;83:956
Activating parabrachial cannabinoid CB1 receptors selectively stimulates feeding of palatable foods in rats.
J Neurosci 2008;28:9702
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