Stimulation of mucin biosynthesis in rat gastric mucosa by FRG-8813 and its structural analogs

Eur J Pharmacol. 1996 Feb 15;297(1-2):87-92. doi: 10.1016/0014-2999(95)00731-8.

Abstract

Certain chemical properties, which may determine the stimulatory actions of the new histamine H2 receptor antagonist, FRG-8813 (2-(furfurylsulfinyl)-N-(4-[4-(piperidinomethyl)-2-pyridyl]o xy-(Z)- 2-butenyl)acetamide), on mucin biosynthesis, were identified by considering the derivation of this drug using an organ culture system of the rat stomach. [3H]Glucosamine and [35S]sulfate incorporation was stimulated in the corpus region by FRG-8813 and its structural analog, compound A (N-[4-[[4- (piperidinylmethyl)pyridyl]-2-oxy]-(Z)-2-butenyl]phthalimide). The chronotropic response to histamine in the guinea pig right atria was suppressed by FRG-8813 in a concentration-dependent fashion. In contrast, compound A did not suppress the histamine-induced response. Ranitidine at 10(-4) M did not suppress the FRG-8813-induced increase in [3H]glucosamine incorporation into mucin. These results suggest that the pyridine derivative and amide structure are chemically important in FRG-8813 as a stimulant on mucus metabolism. Also, this effect is not directly due to histamine H2 receptor antagonism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / pharmacology*
  • Animals
  • Gastric Mucosa / drug effects
  • Gastric Mucosa / metabolism*
  • Heart Atria / drug effects
  • Heart Rate / drug effects
  • Histamine H2 Antagonists / pharmacology*
  • Male
  • Mucins / biosynthesis*
  • Organ Culture Techniques
  • Piperidines / pharmacology*
  • Proteins / metabolism
  • Pyloric Antrum / metabolism
  • Pyridines / pharmacology*
  • Rats
  • Rats, Wistar

Substances

  • Acetamides
  • Histamine H2 Antagonists
  • Mucins
  • Piperidines
  • Proteins
  • Pyridines
  • lafutidine