Effect of endothelin on bladder contraction: potential role in bladder hyperactivity

Pharmacology. 2003 Sep;69(1):7-11. doi: 10.1159/000071243.

Abstract

In the present study, we demonstrate that the intravenous infusion of endothelin-1 (3 and 10 ng/kg/min) causes a decrease in the mean micturition volume of rats in addition to an increase in mean arterial pressure. These effects are blocked by both the ET(A)/ET(B)-non-selective and the ET(A)-selective endothelin antagonists SB 217242 and SB 247083 respectively (both 30 mg/kg). However, it was also observed that the ET(B)-selective agonist sarafotoxin 6c (3 and 10 ng/kg/min) had similar effects on both mean arterial pressure and micturition volume. Initial experiments indicated that spontaneously hypertensive rats have a much lower mean micturition volume than normal rats. Binding studies comparing the total number and ratio of ET(A)/ET(B) receptors in spontaneously hypertensive, Wister-Kyoto and Sprague-Dawley rats revealed no significant differences in receptor expression. However, the magnitude of the response to endothelin-1 was greater in spontaneously hypertensive versus normal rats.

MeSH terms

  • Animals
  • Benzofurans / pharmacology
  • Carboxylic Acids / pharmacology
  • Dose-Response Relationship, Drug
  • Endothelins / pharmacology*
  • Hypertension / chemically induced
  • Hypertension / complications
  • Hypertension / physiopathology
  • Indans / pharmacology
  • Infusions, Intravenous
  • Male
  • Muscle Contraction / drug effects
  • Propionates / pharmacology
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred WKY
  • Rats, Sprague-Dawley
  • Urinary Bladder / physiology*
  • Urination / drug effects
  • Urination Disorders / chemically induced
  • Urination Disorders / physiopathology

Substances

  • Benzofurans
  • Carboxylic Acids
  • Endothelins
  • Indans
  • Propionates
  • SB 247083
  • enrasentan