Is there correlation between analgesic potency and biodegradation of enkephalin analogs?

Sándor Bajusz, András Patthy, Ágnes Kenessey, L. Gráf, József I. Székely, A. Rónai

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Met-enkephalin and its Pro5 analogs containing Gly or D amino acids at position 2 were subjected to digestion with aminopeptidase M, rat brain extracts and human sera. The enzyme resistance of these peptides was compared with their analgesic activity determined in tail flick test after central and intravenous administrations. Our data did not reveal an unambigous correlation between the analgesic potency and metabolic stability of the analogs. This suggest that analgesic activity of synthetic peptides should be due to factors other than enzyme resistance /e.g. receptor binding and transport properties/.

Original languageEnglish
Pages (from-to)1045-1053
Number of pages9
JournalBiochemical and Biophysical Research Communications
Volume84
Issue number4
DOIs
Publication statusPublished - Oct 30 1978

Fingerprint

Enkephalins
Biodegradation
Analgesics
CD13 Antigens
Methionine Enkephalin
Peptides
Enzymes
Intravenous Administration
Transport properties
Tail
Rats
Digestion
Brain
Amino Acids
Serum

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Is there correlation between analgesic potency and biodegradation of enkephalin analogs? / Bajusz, Sándor; Patthy, András; Kenessey, Ágnes; Gráf, L.; Székely, József I.; Rónai, A.

In: Biochemical and Biophysical Research Communications, Vol. 84, No. 4, 30.10.1978, p. 1045-1053.

Research output: Contribution to journalArticle

Bajusz, Sándor ; Patthy, András ; Kenessey, Ágnes ; Gráf, L. ; Székely, József I. ; Rónai, A. / Is there correlation between analgesic potency and biodegradation of enkephalin analogs?. In: Biochemical and Biophysical Research Communications. 1978 ; Vol. 84, No. 4. pp. 1045-1053.
@article{fbf778cdba2b464f963d57b41a15fb31,
title = "Is there correlation between analgesic potency and biodegradation of enkephalin analogs?",
abstract = "Met-enkephalin and its Pro5 analogs containing Gly or D amino acids at position 2 were subjected to digestion with aminopeptidase M, rat brain extracts and human sera. The enzyme resistance of these peptides was compared with their analgesic activity determined in tail flick test after central and intravenous administrations. Our data did not reveal an unambigous correlation between the analgesic potency and metabolic stability of the analogs. This suggest that analgesic activity of synthetic peptides should be due to factors other than enzyme resistance /e.g. receptor binding and transport properties/.",
author = "S{\'a}ndor Bajusz and Andr{\'a}s Patthy and {\'A}gnes Kenessey and L. Gr{\'a}f and Sz{\'e}kely, {J{\'o}zsef I.} and A. R{\'o}nai",
year = "1978",
month = "10",
day = "30",
doi = "10.1016/0006-291X(78)91689-3",
language = "English",
volume = "84",
pages = "1045--1053",
journal = "Biochemical and Biophysical Research Communications",
issn = "0006-291X",
publisher = "Academic Press Inc.",
number = "4",

}

TY - JOUR

T1 - Is there correlation between analgesic potency and biodegradation of enkephalin analogs?

AU - Bajusz, Sándor

AU - Patthy, András

AU - Kenessey, Ágnes

AU - Gráf, L.

AU - Székely, József I.

AU - Rónai, A.

PY - 1978/10/30

Y1 - 1978/10/30

N2 - Met-enkephalin and its Pro5 analogs containing Gly or D amino acids at position 2 were subjected to digestion with aminopeptidase M, rat brain extracts and human sera. The enzyme resistance of these peptides was compared with their analgesic activity determined in tail flick test after central and intravenous administrations. Our data did not reveal an unambigous correlation between the analgesic potency and metabolic stability of the analogs. This suggest that analgesic activity of synthetic peptides should be due to factors other than enzyme resistance /e.g. receptor binding and transport properties/.

AB - Met-enkephalin and its Pro5 analogs containing Gly or D amino acids at position 2 were subjected to digestion with aminopeptidase M, rat brain extracts and human sera. The enzyme resistance of these peptides was compared with their analgesic activity determined in tail flick test after central and intravenous administrations. Our data did not reveal an unambigous correlation between the analgesic potency and metabolic stability of the analogs. This suggest that analgesic activity of synthetic peptides should be due to factors other than enzyme resistance /e.g. receptor binding and transport properties/.

UR - http://www.scopus.com/inward/record.url?scp=0018083111&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0018083111&partnerID=8YFLogxK

U2 - 10.1016/0006-291X(78)91689-3

DO - 10.1016/0006-291X(78)91689-3

M3 - Article

C2 - 728144

AN - SCOPUS:0018083111

VL - 84

SP - 1045

EP - 1053

JO - Biochemical and Biophysical Research Communications

JF - Biochemical and Biophysical Research Communications

SN - 0006-291X

IS - 4

ER -