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

Rónai András

Timár Júlia

Mako E

Erdő Franciska

Gyarmati Zsuzsanna

Tóth Géza

Orosz György

Fürst Zsuzsanna

Székely József Iván

1998

03.01.06. Farmakológia és gyógyszerészet

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.

angol

angol

Folyóiratcikk

PeerReviewed

text

https://publikacio.ppke.hu/id/eprint/2338/1/lifescience1999.pdf

Rónai András; Timár Júlia; Mako E; Erdő Franciska; Gyarmati Zsuzsanna; Tóth Géza; Orosz György; Fürst Zsuzsanna; 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)

MTMT:117447 10.1016/S0024-3205(98)00544-X

https://publikacio.ppke.hu/id/eprint/2338/

https://doi.org/10.1016/S0024-3205%2898%2900544-X

MTMT:117447 10.1016/S0024-3205(98)00544-X