Vardenafil-d₅

Vardenafil-d₅ is intended for use as an internal standard for the quantification of vardenafil (Item No. 14930) 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.

WARNING This product is not for human or veterinary use.

1. Card, G.L., England, B.P., Suzuki, Y., et al. Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12(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 ED. Bioorg. 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 adherence. Int. 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 dysfunction. J. 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 mice. Behav. Brain Res. 253, 103-112 (2013).