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Studies on analgesic oligopeptides. VII. Solid phase synthesis and biological properties of Tyr-D-Arg-Phe-beta Ala-NH2 and its fluorinated aromatic amino acid derivatives.

Authors
  • Sasaki, Y
  • Ambo, A
  • Suzuki, K
Type
Published Article
Journal
Chemical & pharmaceutical bulletin
Publication Date
Sep 01, 1991
Volume
39
Issue
9
Pages
2316–2318
Identifiers
PMID: 1804544
Source
Medline
License
Unknown

Abstract

Tyr-D-Arg-Phe-beta Ala-NH2 (I) and its six fluorinated analogs were synthesized. Their opioid receptor binding properties were examined in vitro and their analgesic activity in vivo using the mouse writhing test. It was found that I was one of the most selective and potent mu-receptor agonists reported to date. [Tyr(2F)1](VI) and [Tyr(3F)1](V) derivatives of I showed similar biological properties to those of I. Since these peptides resist enzymatic degradation, it is expected that they are excellent reagents for the studies of function of mu-receptor-mediated biological properties in vivo and in vitro.

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