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.
Certificate of Analysis / Safety Data Sheet
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.
Kramer et al (1989) Novel peptidic mu opioid antagonists: pharmacologic characterization in vitro and in vivo. J.Pharmacol.Exp.Ther. 249 544. PMID: 2566679.
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.
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Keywords: CTAP, supplier, Selective, potent, μ-opioid, mu-opioid, antagonists, MOP, Receptors, OP3
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