The antisecretory effects of somatostatin and analogues in rat descending colon mucosa

Eur J Pharmacol. 1990 Aug 10;184(2-3):295-303. doi: 10.1016/0014-2999(90)90621-c.

Abstract

Somatostatin-14 (SS-14) and somatostatin-28 (SS-28) produce concentration dependent reductions in short-circuit current in rat colonic mucosa. EC50 values of 15.0 and 13.3 nM were obtained for SS-14 and SS-28 respectively while the N-terminal fragments of SS-28, namely somatostatin-(1-12) (SS1-12) and somatostatin-(1-14) (SS1-14) were inactive. Cyclo(Pro-Phe-D-Trp-Lys-Thr-Phe) and cyclo(Pro-Tyr-D-Trp-Lys-Thr-Phe) were potent antisecretory peptides, like SS-14 and SS-28; while the putative somatostatin antagonist, cyclo(7-aminoheptanoyl-Phe-D-Trp-Lys-Thr[Bzl]) exhibited neither agonist nor antagonist effects. Responses to SS-14 could be regulated by agents which affected the secretory state of the epithelium. Antisecretory effects of SS-14 were markedly attenuated by piroxicam and were restored following piroxicam plus either forskolin or vasoactive intestinal polypeptide (VIP). SS-14 also attenuated secretory responses produced by carbachol, substance P (SP), VIP and alpha- and beta-calcitonin gene related peptide (alpha-, beta-CGRP). Therefore, SS-14 exhibits broad spectrum antisecretory effects in rat descending colon mucosa.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcitonin Gene-Related Peptide / pharmacology
  • Carbachol / pharmacology
  • Colforsin / pharmacology
  • Colon / drug effects*
  • In Vitro Techniques
  • Intestinal Mucosa / drug effects*
  • Intestinal Mucosa / metabolism
  • Male
  • Molecular Sequence Data
  • Piroxicam / pharmacology
  • Protein Precursors / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Somatostatin / analogs & derivatives*
  • Somatostatin / antagonists & inhibitors
  • Somatostatin / pharmacology*
  • Somatostatin-28
  • Substance P / pharmacology
  • Tetrodotoxin / pharmacology
  • Vasoactive Intestinal Peptide / pharmacology
  • ortho-Aminobenzoates / pharmacology

Substances

  • Protein Precursors
  • ortho-Aminobenzoates
  • Piroxicam
  • Colforsin
  • Substance P
  • Vasoactive Intestinal Peptide
  • Tetrodotoxin
  • Somatostatin
  • Somatostatin-28
  • Carbachol
  • fenamic acid
  • Calcitonin Gene-Related Peptide