Tetrapeptide-amide analogues of enkephalin: The role of C-terminus in determining the character of opioid activity

A. Rónai, J. I. Székely, I. Berzétei, E. Miglécz, S. Bajusz

Research output: Article

31 Citations (Scopus)

Abstract

The opioid activities of tetrapeptide-amide analogues of enkephalin /H-Tyr-D-Met-Gly-Phe-NH2; H-Tyr-D-Nle-Gly-Phe-NH2/ were studied in isolated, electrically stimulated longitudinal muscle strip of guinea-pig ileum and mouse vas deferens preparations in vitro and in vivo in the rat tail-flick test. Their effects were compared to those of the parent L-Pro5-NH2 containing analogues, and to other enkephalin derivatives substituted with D-Met in position 2 and L-amino/imino acids of different character in position 5. It was found that whilst the opioid receptor in mouse vas deferens preferred aliphatic residues of acidic character at the C-terminus of pentapeptides and was highly sensitive to the removal of C-terminal amino acid, the other systems were either much less responsive to these changes, or the effects were opposite to those found in mouse vas deferens.

Original languageEnglish
Pages (from-to)1239-1249
Number of pages11
JournalBiochemical and Biophysical Research Communications
Volume91
Issue number4
DOIs
Publication statusPublished - dec. 28 1979

Fingerprint

Vas Deferens
Enkephalins
Amides
Opioid Analgesics
Imino Acids
glycylphenylalanine
Opioid Receptors
Muscle
Rats
Amino Acids
Derivatives
Ileum
Tail
Guinea Pigs
Muscles

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Tetrapeptide-amide analogues of enkephalin : The role of C-terminus in determining the character of opioid activity. / Rónai, A.; Székely, J. I.; Berzétei, I.; Miglécz, E.; Bajusz, S.

In: Biochemical and Biophysical Research Communications, Vol. 91, No. 4, 28.12.1979, p. 1239-1249.

Research output: Article

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