Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities

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 activi...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-09, Vol.23 (17), p.4975-4978
Hauptverfasser:	Nair, Padma, Yamamoto, Takashi, Largent-Milnes, Tally M., Cowell, Scott, Kulkarni, Vinod, Moye, Sharif, Navratilova, Edita, Davis, Peg, Ma, Shou-Wu, Vanderah, Todd W., Lai, Josephine, Porreca, Frank, Hruby, Victor J.
Format:	Artikel
Sprache:	eng
Schlagworte:	agonists Amino Acid Sequence amino acid sequences Analgesics - chemistry Analgesics - pharmacology Analgesics - therapeutic use Animals antagonists Bifunctional compounds Humans Ligands Neurokinin-1 Receptor Antagonists - chemistry Neurokinin-1 Receptor Antagonists - pharmacology Neurokinin-1 Receptor Antagonists - therapeutic use Neutokinin-1 receptor antagonists NMR structure Opioid receptor agonists Peptides - chemistry Peptides - pharmacology Peptides - therapeutic use Rats Receptors, Neurokinin-1 - metabolism Receptors, Opioid, delta - agonists Receptors, Opioid, delta - metabolism Receptors, Opioid, mu - agonists Receptors, Opioid, mu - metabolism substance P Truncation of peptide sequence
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.06.065