Reference
Nair, Padma, et al. “Truncation of the Peptide Sequence in Bifunctional Ligands With Mu and Delta Opioid Receptor Agonist and Neurokinin 1 Receptor Antagonist Activities”. Bioorg Med Chem Lett, vol. 23, no. 17, Jan. 2013, pp. 4975-8, https://doi.org/10.1016/j.bmcl.2013.06.065.
Abstract
The optimization and truncation of our lead peptide-derived ligand TY005 possessing eight amino-acid residues was performed. Among the synthesized derivatives, NP30 (Tyr(1)-DAla(2)-Gly(3)-Phe(4)-Gly(5)-Trp(6)-O-[3',5'-Bzl(CF3)2]) showed balanced and potent opioid agonist as well as substance P antagonist activities in isolated tissue-based assays, together with significant antinociceptive and antiallodynic activities in vivo.