A comparative study of sildenafil, NCX-911 and BAY41-2272 on the anococcygeus muscle of diabetic rats

Int J Impot Res. 2004 Dec;16(6):479-85. doi: 10.1038/sj.ijir.3901224.

Abstract

We compared the effects of a nitric oxide (NO)-releasing sildenafil (NCX-911), NO-independent soluble guanylate cyclase activator (BAY41-2272) and sildenafil on the anococcygeus muscle from streptozotocin-induced 16-weeks diabetic rats. NCX-911, BAY41-2272 and sildenafil reduced the phenylephrine-induced tone in the control group (EC50=1088.8+/-165.0, 151.6+/-9.3 and 827.1+/-167.3 nM, respectively). The potencies of NCX-911 and BAY41-2272 were not altered, but that of sildenafil was significantly reduced in the diabetic group. EC50 values for NCX-911, BAY41-2272 and sildenafil in the diabetic group were 1765.9+/-303.5, 209.7+/-27.3 and 2842.2+/-640.3 nM, respectively (P<0.05 for sildenafil). Nitrergic relaxation responses were significantly decreased in the diabetic group. The remaining nitrergic relaxation responses were potentiated by BAY41-2272 but not by sildenafil or NCX-911. These results confirm that endogenous NO derived from nitrergic nerves is significantly decreased in diabetes, and suggest that NO-releasing PDE5 inhibitors and NO-independent soluble guanylate cyclase activators could be more useful than PDE5 inhibitors in the treatment of ED in long-term diabetes.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Anal Canal
  • Animals
  • Diabetes Mellitus, Experimental / physiopathology*
  • Electric Stimulation
  • Male
  • Muscle Relaxation / drug effects
  • Muscles / drug effects*
  • Muscles / innervation
  • Nitrergic Neurons / drug effects
  • Nitrergic Neurons / physiology
  • Phenylephrine / pharmacology
  • Phosphodiesterase Inhibitors / pharmacology
  • Piperazines / pharmacology*
  • Purines
  • Pyrazoles / pharmacology*
  • Pyridines / pharmacology*
  • Rats
  • Rats, Wistar
  • Sacrococcygeal Region
  • Sildenafil Citrate
  • Sulfones

Substances

  • 3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo(3,4-b)pyridine
  • Adrenergic alpha-Agonists
  • Phosphodiesterase Inhibitors
  • Piperazines
  • Purines
  • Pyrazoles
  • Pyridines
  • Sulfones
  • Phenylephrine
  • Sildenafil Citrate