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:
  • Formula:
  • Sequence:

    (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:
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
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