We have developed a novel series of peptides, related to the NKA(4-10) sequence, in which substitution of selected amino acids determined variations in the affinity for the TK receptor subtypes. Subcutaneous pretreatment of rats with some peptides of this series reduced gastric ulcers induced by ethanol, indomethacin or acetylsalicyclic acid (ASA) as well as duodenal ulcers induced by dulcerozine. In particular [Ala5]NKA(4-10) and [Ala5,βAla8]NKA(4-10) possess a broad spectrum of antiulcer activity which is long lasting and stronger than the precursor NKA(4-10). The observation that the prevention of ethanol-induced gastric lesions could be reversed by pretreatment with indomethacin favors the possible involvement of prostaglandins in the observed gastroprotection by TK analogs.
Analogs of neurokinin A(4-10) afford protection against gastroduodenal ulcers in rats / Stefano Evangelista; Carlo A. Maggi; Paolo Rovero; Riccardo Patacchini; Sandro Giuliani; Antonio Giachetti. - In: PEPTIDES. - ISSN 0196-9781. - STAMPA. - 11 (2):(1990), pp. 293-297.
Analogs of neurokinin A(4-10) afford protection against gastroduodenal ulcers in rats
ROVERO, PAOLO;
1990
Abstract
We have developed a novel series of peptides, related to the NKA(4-10) sequence, in which substitution of selected amino acids determined variations in the affinity for the TK receptor subtypes. Subcutaneous pretreatment of rats with some peptides of this series reduced gastric ulcers induced by ethanol, indomethacin or acetylsalicyclic acid (ASA) as well as duodenal ulcers induced by dulcerozine. In particular [Ala5]NKA(4-10) and [Ala5,βAla8]NKA(4-10) possess a broad spectrum of antiulcer activity which is long lasting and stronger than the precursor NKA(4-10). The observation that the prevention of ethanol-induced gastric lesions could be reversed by pretreatment with indomethacin favors the possible involvement of prostaglandins in the observed gastroprotection by TK analogs.I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.