Effect of NS-21, an anticholinergic drug with calcium antagonistic activity, on lower urinary tract function in a rat model of urinary frequency

Int J Urol. 1997 Jul;4(4):401-6. doi: 10.1111/j.1442-2042.1997.tb00215.x.

Abstract

Background: NS-21 is under development for the treatment of urinary frequency and urinary incontinence. The purpose of this study was to investigate the effects of NS-21 and its active metabolite, RCC-36, on lower urinary tract function in an experimental rat model of urinary frequency.

Methods: Cystometrograms were recorded in anesthetized rats with bilaterally transected hypogastric nerves. All drugs were administered intraduodenally.

Results: In sham-operated rats, NS-21 (> or = 50 mg/kg) significantly increased the bladder capacity without significantly decreasing micturition pressure, while RCC-36 (100 mg/kg) significantly increased bladder capacity, and at a dose of > or = 30 mg/kg, also caused a decrease in micturition pressure. This increase in bladder capacity appeared at lower doses of both NS-21 and RCC-36 in the hypogastric nerve-transected rats. Propiverine (100 mg/kg) increased bladder capacity and at > or = 30 mg/kg, decreased micturition pressure in both sham-operated and nerve-transected rats. Oxybutynin (100 mg/kg) and atropine (30 mg/kg) decreased the micturition pressure in both sham-operated and nerve-transected rats without increasing the bladder capacity, while a similar anticholinergic calcium antagonist, terodiline (100 mg/kg) had no effect on bladder capacity in either sham-operated or nerve-transected rats. Flavoxate (500 mg/kg) significantly increased bladder capacity without significantly decreasing micturition pressure in both sham-operated and nerve-transected rats, while 50 mg/kg of verapamil significantly increased bladder capacity without significantly decreasing the micturition pressure in nerve-transected rats.

Conclusions: NS-21 and RCC-36 increased bladder capacity at lower doses in hypogastric nerve-transected rats than in sham-operated rats. Furthermore, NS-21 increased the bladder capacity without suppressing micturition pressure, suggesting that NS-21 may be a more effective therapeutic drug than propiverine, oxybutynin or flavoxate for the treatment of urinary frequency and urinary incontinence.

MeSH terms

  • Animals
  • Atropine / pharmacology
  • Benzilates / pharmacology
  • Calcium Channel Blockers / pharmacology*
  • Denervation
  • Disease Models, Animal
  • Flavoxate / pharmacology
  • Hypogastric Plexus / surgery
  • Male
  • Mandelic Acids / pharmacology
  • Parasympatholytics / pharmacology
  • Phenylacetates / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Urinary Bladder / chemistry
  • Urinary Bladder / drug effects
  • Urinary Incontinence / drug therapy*

Substances

  • Benzilates
  • Calcium Channel Blockers
  • Mandelic Acids
  • Parasympatholytics
  • Phenylacetates
  • RCC 36
  • Flavoxate
  • propiverine
  • Atropine
  • temiverine
  • oxybutynin