CTAP

Description: Potent and selective µ opioid receptor antagonist (IC50 = 3.5 nM). Displays > 1200-fold selectivity over delta opioid and somatostatin receptors. Brain penetrant and active in vivo. Smiles: C[C@@H](O)[C@H](NC(=O)C1NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CSSC1(C)C)NC(=O)[C@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O. References: Abbruscato et al (1997) Blood-brain barrier permeability and bioavailability of a highly potent and µ-selective opioid receptor antagonist, CTAP: comparison with mor. J.Pharmacol.Exp.Ther. 280 402 PMID: