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

Rónai András and Timár Júlia and Mako E and Erdő Franciska and Gyarmati Zsuzsanna and Tóth Géza and Orosz György and Fürst Zsuzsanna and Székely József Iván: Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV (EC3.4.14.5) produces naloxone-reversible analgesia in rats.
LIFE SCIENCES, 64 (2). pp. 145-152. ISSN 0024-3205 (1998)

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Item Type:

Article

Creators:

Creators	ORCID	MTMT szerző azonosító
Rónai András		51
Timár Júlia	0000-0003-3511-7607	10006033
Mako E
Erdő Franciska		10044620
Gyarmati Zsuzsanna		10015478
Tóth Géza		10005935
Orosz György		10007647
Fürst Zsuzsanna	0000-0002-2760-1274	10005121
Székely József Iván		10004208

Abstract:

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.

Journal or Publication Title:

LIFE SCIENCES

Date:

1998

Volume:

Number:

Page Range:

pp. 145-152

ISSN:

0024-3205

Institution:

Pázmány Péter Katolikus Egyetem