Analogs of neurokinin A(4-10) afford protection against gastroduodenal ulcers in rats.

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 acetylsalicylic acid (ASA) as well as duodenal ulcers induced by dulcerozine. In particular [Ala5]NKA(4-10) and [Ala5,beta Ala8]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.

• Authors: S Evangelista, C A Maggi, P Rovero, R Patacchini, S Giuliani, A Giachetti
• Journal: Peptides (Peptides) 1990 Mar-Apr Vol. 11 Issue 2 Pg. 293-7 ISSN: 0196-9781 [Print] United States
• PMID: 2162531 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Peptide Fragments
• Receptors, Neurotransmitter
• Receptors, Tachykinin
• Neurokinin A
• neurokinin A(4-10)

Topics

• Amino Acid Sequence
• Analysis of Variance
• Animals
• Female
• Male
• Molecular Sequence Data
• Neurokinin A (metabolism, pharmacology)
• Peptic Ulcer (prevention & control)
• Peptide Fragments (metabolism, pharmacology)
• Premedication
• Rats
• Rats, Inbred Strains
• Receptors, Neurotransmitter (metabolism)
• Receptors, Tachykinin