Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV (EC3.4.14.5) produces naloxone-reversible analgesia in rats

The dipeptidyl aminopeptidase IV (DP IV) inhibitor Diprotin A produces st full, dose-dependent, short-lasting and naloxone- reversible analgesia in the rat tail-flick test when given intracerebroventricularly, with an ED50 of 295 nmol/rat but it has no direct opioid agonist activity in the longit...

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Bibliographic Details
Main Authors: Rónai András
Timár Júlia
Mako E
Erdő Franciska
Gyarmati Zsuzsanna
Tóth Géza
Orosz György
Fürst Zsuzsanna
Székely József Iván
Format: Article
Published: 1998
Series:LIFE SCIENCES 64 No. 2
Subjects:
Farmakológia és gyógyszerészet
doi:10.1016/S0024-3205(98)00544-X

mtmt:117447
Online Access:https://publikacio.ppke.hu/2338
Description
Summary:The dipeptidyl aminopeptidase IV (DP IV) inhibitor Diprotin A produces st full, dose-dependent, short-lasting and naloxone- reversible analgesia in the rat tail-flick test when given intracerebroventricularly, with an ED50 of 295 nmol/rat but it has no direct opioid agonist activity in the longitudinal muscle strip of guinea-pig ileum bioassay. Two of the potential DP IV substrates, morphiceptin and endomorphin 1, identified recently in bovine brain were also analgesic given by similar route. The action of endomorphin 1 was more potent (ED50 = 7.9 nmol/rat) and slightly but significantly more sustained than that of Diprotin A. Diprotin A neither potentiated nor prolonged the effect of a marginally analgesic dose of endomorphin 1. The distinct time course and the lack of potentiation indicate that in the analgesic effect of Diprotin A. in rats the protection of a brain Tyr-Pro-peptide other than endomorphin 1 is involved.
Physical Description:145-152
ISSN:0024-3205

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