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Titolo:
Antisecretory and gastroprotective activities of compounds endowed with H-2 antagonistic and nitric oxide (NO) donor properties
Autore:
Coruzzi, G; Adami, M; Morini, G; Pozzoli, C; Cena, C; Bertinaria, M; Gasco, A;
Indirizzi:
Univ Parma, Inst Pharmacol, I-43100 Parma, Italy Univ Parma Parma Italy I-43100 rma, Inst Pharmacol, I-43100 Parma, Italy Univ Turin, Dept Sci & Drug Tecnol, I-10125 Turin, Italy Univ Turin Turin Italy I-10125 t Sci & Drug Tecnol, I-10125 Turin, Italy
Titolo Testata:
JOURNAL OF PHYSIOLOGY-PARIS
fascicolo: 1, volume: 94, anno: 2000,
pagine: 5 - 10
SICI:
0928-4257(200001/02)94:1<5:AAGAOC>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
GASTRIC-ACID SECRETION; RAT; MUCOSA; INJURY; PREVENTION; INHIBITOR; INDUCTION; DEFENSE;
Keywords:
histamine H-2 antagonists; nitric oxide; gastric acid secretion; gastroprotection;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Coruzzi, G Univ Parma, Inst Pharmacol, Via Volturno 39, I-43100 Parma, Italy Univ Parma Via Volturno 39 Parma Italy I-43100 00 Parma, Italy
Citazione:
G. Coruzzi et al., "Antisecretory and gastroprotective activities of compounds endowed with H-2 antagonistic and nitric oxide (NO) donor properties", J PHYSL-PAR, 94(1), 2000, pp. 5-10

Abstract

In spite of the well recognized gastric antisecretory activity, the gastroprotective potential of histamine H-2 receptor antagonists is controversial. Most clinical studies in fact indicate that these drugs do not substantially protect the gastric mucosa from aggressive factors. Nitric oxide (NO) has been recently recognized as a fundamental mediator in gastric defence mechanisms, due to its ability to increase gastric mucosal blood flow and mucus production and to inhibit neutrophils adherence to endothelial cells. The aim of this study was to investigate the gastroprotective and H-2 receptor antagonistic activity of a series of lamtidine analogues which contain different NO-releasing moieties (furoxan, nitroxy and nitrosothioI). These compounds were tested, in comparison with related H-2 antagonists devoid of NO-donor structures, in different H-2 receptor assays and in the conscious rat against 0.6 N HCl-induced gastric lesions. All the compounds tested wereable to antagonize histamine-mediated responses at cardiac and gastric H-2receptors; however, furoxan and nitroxy derivatives were 10-fold less potent than the analogues devoid of NO-donor properties. By contrast, NO-donor compounds were more active than reference Il, antagonists as gastroprotective agents against mucosal injury induced by 0.6 N HCl. Among the different NO-donor moieties, the furoxan group conferred to the H-2 antagonist molecule the highest gastroprotective potential; this finding closely correlates with the characteristics of NO release. In conclusions, lamtidine-analogue H-2 antagonists combined with NO-donor moieties are endowed with gastric antisecretory and protective activity and could be the prototypes of a new class of anti-ulcer drugs. Finally, the furoxan NO donor group seems to be the most favourable among the different moieties tested. (C) 2000 Elsevier Science Ltd. Published by Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/06/20 alle ore 01:34:15