CTAP
Purity: ≥95%
Biological Activity
CTAP 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.Technical Data
(Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = 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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Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo.
Kramer et al.
J.Pharmacol.Exp.Ther., 1989;249:544 -
Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors.
Pelton et al.
J.Med.Chem., 1986;29:2370 -
Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with mor.
Abbruscato et al.
J.Pharmacol.Exp.Ther., 1997;280:402
Product Datasheets
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Citations for CTAP
The citations listed below are publications that use Tocris products. Selected citations for CTAP include:
13 Citations: Showing 1 - 10
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Synapse-specific opioid modulation of thalamo-cortico-striatal circuits.
Authors: Birdsong Et al.
Elife 2019;8
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MOR-Induced Modulation of Endolysosomal Iron Mediates Upregulation of Ferritin Heavy Chain in Cortical Neurons.
Authors: Nash Et al.
Eneuro 2019;6
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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
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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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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
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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
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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
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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
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Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation.
Authors: Krook-Magnuson Et al.
J Neurosci 2011;31:14861
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Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5.
Authors: Song Et al.
J Biol Chem 2011;286:20354
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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
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DAMGO-induced expression of chemokines and chemokine receptors: the role of TGF-β1.
Authors: Happel Et al.
Front Cell Neurosci 2008;83:956
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Activating parabrachial cannabinoid CB1 receptors selectively stimulates feeding of palatable foods in rats.
Authors: DiPatrizio
J Neurosci 2008;28:9702
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