Catalog Number: 1560
Biological Activity
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
  • M.Wt:
    1104.32
  • Formula:
    C51H69N13O11S2
  • Sequence:
    FCYWRTXT

    (Modifications: Phe-1 = D-Phe, Trp-4 = D-Trp, X = Pen, Disulfide bridge between 2 - 7, Thr-8 = C-terminal amide)

  • Solubility:
    Soluble to 1 mg/ml in water
  • Storage:
    Desiccate at -20°C
  • CAS No:
    103429-32-9
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.
Background References
  1. Blood-brain barrier permeability and bioavailability of a highly potent and μ-selective opioid receptor antagonist, CTAP: comparison with morphine.
    Abbruscato et al.
    J.Pharmacol.Exp.Ther., 1997;280:402
  2. Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo.
    Kramer et al.
    J.Pharmacol.Exp.Ther., 1989;249:544
  3. 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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for CTAP include:

5 Citations: Showing 1 - 5
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  1. Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude.
    Authors: Gerhold Et al.
    J Neurosci 2015;35:9580
  2. Ivy and neurogliaform interneurons are a major target of μ-opioid receptor modulation.
    Authors: Krook-Magnuson Et al.
    J Neurosci 2011;31:14861
  3. Protein kinase Czeta mediates micro-opioid receptor-induced cross-desensitization of chemokine receptor CCR5.
    Authors: Song Et al.
    J Biol Chem 2011;286:20354
  4. 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
  5. 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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