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Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities |
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| Authors: | Padma Nair Takashi Yamamoto Tally M Largent-Milnes Scott Cowell Vinod Kulkarni Sharif Moye Edita Navratilova Peg Davis Shou-Wu Ma Todd W Vanderah Josephine Lai Frank Porreca Victor J Hruby |
| Institution: | 1. Department of Chemistry and Biochemistry, University of Arizona, 1306 East University Boulevard, Tucson, AZ 85721, USA;2. Department of Pharmacology, University of Arizona, 1501 North Campbell Avenue, Tucson, AZ 85724, USA |
| Abstract: | The optimization and truncation of our lead peptide-derived ligand TY005 possessing eight amino-acid residues was performed. Among the synthesized derivatives, NP30 (Tyr1-DAla2-Gly3-Phe4-Gly5-Trp6-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. |
| Keywords: | Bifunctional compounds Opioid receptor agonists Neutokinin-1 receptor antagonists Truncation of peptide sequence NMR structure |
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