Cat. No. 1560
Biological ActivityPotent 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 between 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.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Abbruscato et al (1997) Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with morphine. J.Pharmacol.Exp.Ther. 280 402. PMID: 8996221.
Kramer et al (1989) Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo. J.Pharmacol.Exp.Ther. 249 544. PMID: 2566679.
Pelton et al (1986) Design and synthesis of conformationally constrained somatostatin analogues with high potency and specificity for μ opioid receptors. J.Med.Chem. 29 2370. PMID: 2878079.
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Citations are publications that use Tocris products. Selected citations for CTAP include:
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.
Krook-Magnuson et al (2011) Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation. J Neurosci 31 14861. PMID: 22016519.
Song et al (2011) Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5. J Biol Chem 286 20354. PMID: 21454526.
Sengupta et al (2009) Morphine increases brain levels of ferritin heavy chain leading to inhibition of CXCR4-mediated survival signaling in neurons. J Leukoc Biol 29 2534. PMID: 19244528.
Happel et al (2008) DAMGO-induced expression of chemokines and chemokine receptors: the role of TGF-β1. Front Cell Neurosci 83 956. PMID: 18252865.
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Keywords: CTAP, supplier, Selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3, Tocris Bioscience, μ Opioid Receptor Antagonist products
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