Effects of YM435, a novel dopamine D1 receptor agonist, on pancreatic exocrine secretion in anesthetized dogs

Eur J Pharmacol. 1992 Aug 6;218(2-3):237-41. doi: 10.1016/0014-2999(92)90174-3.

Abstract

The effects of YM435, a novel dopamine (DA) D1 receptor agonist, on pancreatic exocrine secretion were investigated in anesthetized dogs. Each drug was injected i.a. as a single bolus. Graded doses of YM435 (0.3-30 nmol) produced dose-dependent increases in the rate of secretion of pancreatic juice, with a maximum effect at approximately 10 nmol, and with a high concentration of bicarbonate and low concentration of protein. SCH23390 (3-30 nmol), a selective D1 receptor antagonist, caused a progressive parallel shift to the right of the dose-response curve for YM435-stimulated pancreatic secretion without changing the maximum response. Schild analysis of the data indicated that the inhibitory constant (Ki) value was 2.9 nmol, and that SCH23390 inhibited YM435-stimulated pancreatic secretion in a competitive manner. Both DA (0.01-3 mumol) and SKF38393 (0.3-30 mumol), a selective D1 receptor agonist, also increased the secretory rate and bicarbonate concentration, and decreased the protein concentration to the same extent as YM435. These results suggest that YM435 is a potent stimulant of pancreatic exocrine secretion by acting on DA D1 receptors of the pancreas in dogs.

MeSH terms

  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine / pharmacology
  • Animals
  • Benzazepines / pharmacology
  • Dogs
  • Dopamine / pharmacology
  • Dose-Response Relationship, Drug
  • Female
  • Isoquinolines / pharmacology*
  • Male
  • Pancreas / drug effects*
  • Pancreas / metabolism
  • Pancreatic Juice / drug effects
  • Receptors, Dopamine D1 / drug effects*
  • Tetrahydroisoquinolines*

Substances

  • Benzazepines
  • Isoquinolines
  • Receptors, Dopamine D1
  • Tetrahydroisoquinolines
  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
  • zelandopam
  • Dopamine