Discovery of a potent and efficacious peptide derivative for Î´/µ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.

Yamamoto, Takashi; Nair, Padma; Largent-Milnes, Tally M; Jacobsen, Neil E; Davis, Peg; Ma, Shou-Wu; Yamamura, Henry I; Vanderah, Todd W; Porreca, Frank; Lai, Josephine; Hruby, Victor J

Yamamoto, Takashi; Nair, Padma; Largent-Milnes, Tally M; Jacobsen, Neil E; Davis, Peg; Ma, Shou-Wu; Yamamura, Henry I; Vanderah, Todd W; Porreca, Frank; Lai, Josephine; Hruby, Victor J.

Affiliation

Yamamoto T; Department of Chemistry and Biochemistry, University of Arizona, 1306 East University Boulevard, Tucson, Arizona 85721, United States.

J Med Chem ; 54(7): 2029-38, 2011 Apr 14.

Article in En | MEDLINE | ID: mdl-21366266

Subject(s)

Drug Discovery; Neurokinin-1 Receptor Antagonists; Peptides/chemistry; Receptors, Opioid, mu/agonists; Receptors, sigma/agonists; Tyrosine/analogs & derivatives; Amino Acid Sequence; Analgesics/chemistry; Analgesics/metabolism; Analgesics/pharmacology; Animals; Drug Stability; Guanosine 5'-O-(3-Thiotriphosphate)/metabolism; Guinea Pigs; Humans; Ileum/metabolism; Magnetic Resonance Spectroscopy; Male; Mice; Micelles; Molecular Conformation; Rats; Receptors, Neurokinin-1/metabolism; Receptors, Opioid, mu/metabolism; Receptors, sigma/metabolism; Structure-Activity Relationship; Tyrosine/chemistry; Tyrosine/metabolism; Tyrosine/pharmacology; Vas Deferens/metabolism

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Peptides / Tyrosine / Receptors, sigma / Receptors, Opioid, mu / Drug Discovery / Neurokinin-1 Receptor Antagonists Limits: Animals / Humans / Male Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2011 Document type: Article Affiliation country: United States Country of publication: United States

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