Vardenafil-d5 is intended for use as an internal standard for the quantification of vardenafil by GC- or LC-MS. Vardenafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50s = 0.2-1.2 nM) and PDE6 (IC50 = 2 nM).1,2,3 It is selective for PDE5 and PDE6 over PDE1 and PDE11 (IC50s = 230 and 130 nM, respectively). Vardenafil (4 mg/kg per day for three weeks) improves erectile function in a rat model of acute arteriogenic erectile dysfunction by increasing intracavernous pressure and mean arterial pressure, and this effect persists for at least two weeks following the end of treatment.4 Chronic vardenafil administration at a dose of 2 mg/kg for five weeks to subordinate mice reduces the latency to mount and increases the frequency of mounting behavior.5 Formulations containing vardenafil have been used in the treatment of erectile dysfunction.
1.Card, G.L., England, B.P., Suzuki, Y., et al.Structural basis for the activity of drugs that inhibit phosphodiesterasesStructure12(12)2233-2247(2004) 2.Boyle, C.D., Xu, R., Asberom, T., et al.Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male EDBioorg. Med. Chem. Lett.15(9)2365-2369(2005) 3.Smith, W.B., II, McCaslin, I.R., Gokce, A., et al.PDE5 inhibitors: Considerations for preference and long-term adherenceInt. J. Clin. Pract.67(8)768-780(2013) 4.Hotta, Y., Ohno, R., Kataoka, T., et al.Effects of chronic vardenafil treatment persist after end of treatment in rats with acute arteriogenic erectile dysfunctionJ. Sex Med.9(7)1782-1788(2012) 5.Dadomo, H., Parmigiani, S., Nicolini, Y., et al.Repeated and chronic administration of Vardenafil or Sildenafil differentially affects emotional and socio-sexual behavior in miceBehav. Brain Res.253103-112(2013)