Substrate- and inhibitor-specificity of a nonendothelial enzyme which forms [Met5]-enkephalin from [Met5]-enkephalin-Arg6, Phe7 in isolated rabbit ear artery: Pharmacological characterization

A. Rónai, E. Fehér, J. Botyánszki, J. Hepp, A. Magyar, K. Medzihradszky

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The captopril-inhibited enzyme which forms [Met5]-enkephalin from [Met5]-enkephalin-Arg6, Phe7 in isolated rabbit ear artery was characterized further by using various natural substrate candidates/analogues ([Met5]-enkephalin-Arg6, Phe7 and its amide, [Met5]-enkephalin, angiotensin I and bradykinin), peptidase inhibitors such as captopril, enalaprilate and thiorphan and by endothel removal. 10-5 and 10-4 M but not 10-6 M captopril reduced the effectiveness of [Met5]-enkephalin-Arg6,Phe7 and potentiated the effect of bradykinin but did not affect markedly the action of the other peptides. Of the inhibitors, enalaprilate was less effective than captopril, and thiorphan had no effect. The [Met5]-enkephalin-Arg6,Phe7 →[Met5]-enkephalin conversion was not affected by endothel removal. The substrate and inhibitor spectrum of this non-endothelial enzyme activity bears no relationship in other, hitherto characterized dipeptidylcarboxypeptidases/endopeptidases known to be involved in the metabolism of the tested peptides.

Original languageEnglish
Pages (from-to)137-145
Number of pages9
JournalNeuropeptides
Volume28
Issue number3
DOIs
Publication statusPublished - 1995

Fingerprint

Enkephalins
Substrate Specificity
Ear
Arteries
Pharmacology
Rabbits
Captopril
Substrates
Enzymes
Thiorphan
Bradykinin
Angiotensin I
Endopeptidases
Peptides
Enzyme activity
Protease Inhibitors
Metabolism
Amides

ASJC Scopus subject areas

  • Endocrinology
  • Cellular and Molecular Neuroscience
  • Endocrine and Autonomic Systems
  • Neurology
  • Clinical Neurology
  • Endocrinology, Diabetes and Metabolism
  • Neuroscience(all)
  • Biochemistry

Cite this

Substrate- and inhibitor-specificity of a nonendothelial enzyme which forms [Met5]-enkephalin from [Met5]-enkephalin-Arg6, Phe7 in isolated rabbit ear artery : Pharmacological characterization. / Rónai, A.; Fehér, E.; Botyánszki, J.; Hepp, J.; Magyar, A.; Medzihradszky, K.

In: Neuropeptides, Vol. 28, No. 3, 1995, p. 137-145.

Research output: Contribution to journalArticle

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