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Gene Review

PDE5  -  phosphodiesterase isozyme 5

Sus scrofa

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Disease relevance of PDE5


High impact information on PDE5

  • Inhibition of PDE5 by sildenafil was confirmed by elevated S-nitroso-N-acetylpenicillamine-induced cGMP generation in isolated lungs [5].
  • We synthesized various 4-(3-chloro-4-methoxybenzyl)aminophthalazines substituted at the 1- and 6-positions and evaluated their inhibitory activity toward phosphodiesterase 5 (PDE5) and their vasorelaxant activity in isolated porcine coronary arteries precontracted with prostaglandin F2alpha (10(-5) M) [6].
  • 1-Arylnaphthalene lignan, which had been reported as a PDE4 inhibitor by Iwasaki, was disclosed as a new structural class of PDE5 inhibitors [7].
  • These results show that novel PDE5 inhibitors possessing a potent vasorelaxant effect may exist among phthalazine derivatives [8].
  • The PDE5 inhibitors dipyridamole and zaprinast, produced qualitatively similar effects but with lower potency [9].

Biological context of PDE5


Anatomical context of PDE5


Associations of PDE5 with chemical compounds

  • Postnatal maturation of phosphodiesterase 5 (PDE5) in piglet pulmonary arteries: activity, expression, effects of PDE5 inhibitors, and role of the nitric oxide/cyclic GMP pathway [9].
  • In cells made tolerant to SNP, selective PDE5 inhibition synergistically increased intra- and extracellular cGMP amounts after SNP stimulation [10].
  • Four families of PDEs were separated from pig aorta: PDE1 (calcium-calmodulin-activated), PDE3 (cGMP-inhibited), PDE4 (adenosine 3',5'-cyclic monophosphate [cAMP]-specific), and PDE5 (cGMP-specific) [10].
  • Diosmetin more-selectively inhibited PDE2 (IC(50) of 4.8 microM) than PDE1, PDE4, or PDE5 [11].
  • As shown in Table 2, luteolin revealed non-selective inhibition of PDE1-5 with IC(50) values in a range of 10-20 microM, as did genistein except with a low potency on PDE5 [11].

Other interactions of PDE5


Analytical, diagnostic and therapeutic context of PDE5

  • Importantly, our data also show that acute exposure to PDE5 inhibitors for 60 min induces apical accumulation of AQP2 in kidney medullary collecting duct principal cells both in tissue slices incubated in vitro as well as in vivo after intravenous injection of Viagra into rats [12].
  • Employing the established PDE-5 inhibitor sildenafil during lung perfusion, storage, and implantation, ischemic tolerance may be extended and early graft function improved [3].
  • Using a fast protein liquid chromatography system, five PDE isozymes, PDE 1, PDE 2, PDE 3, PDE 4 and PDE 5 were prepared from guinea pig and dog tissues [13].


  1. Phosphodiesterase 5 and effects of sildenafil on cerebral arteries of man and guinea pig. Kruuse, C., Khurana, T.S., Rybalkin, S.D., Birk, S., Engel, U., Edvinsson, L., Olesen, J. Eur. J. Pharmacol. (2005) [Pubmed]
  2. Vardenafil increases coronary flow response to hypercapnic acidosis in isolated guinea pig heart. Brand, M., Deussen, A. Basic Res. Cardiol. (2007) [Pubmed]
  3. Sildenafil extends survival and graft function in a large animal lung transplantation model. Korom, S., Hillinger, S., Cardell, M., Zhai, W., Tan, Q., Dutly, A., Leskosek, B., Weder, W. European journal of cardio-thoracic surgery : official journal of the European Association for Cardio-thoracic Surgery. (2006) [Pubmed]
  4. Signaling molecules in overcirculation-induced pulmonary hypertension in piglets: effects of sildenafil therapy. Rondelet, B., Kerbaul, F., Van Beneden, R., Motte, S., Fesler, P., Hubloue, I., Remmelink, M., Brimioulle, S., Salmon, I., Ketelslegers, J.M., Naeije, R. Circulation (2004) [Pubmed]
  5. Effect of phosphodiesterase-5 inhibitor, sildenafil (Viagra), in animal models of airways disease. Toward, T.J., Smith, N., Broadley, K.J. Am. J. Respir. Crit. Care Med. (2004) [Pubmed]
  6. 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. Watanabe, N., Adachi, H., Takase, Y., Ozaki, H., Matsukura, M., Miyazaki, K., Ishibashi, K., Ishihara, H., Kodama, K., Nishino, M., Kakiki, M., Kabasawa, Y. J. Med. Chem. (2000) [Pubmed]
  7. 1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor. Ukita, T., Nakamura, Y., Kubo, A., Yamamoto, Y., Takahashi, M., Kotera, J., Ikeo, T. J. Med. Chem. (1999) [Pubmed]
  8. 4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. Watanabe, N., Kabasawa, Y., Takase, Y., Matsukura, M., Miyazaki, K., Ishihara, H., Kodama, K., Adachi, H. J. Med. Chem. (1998) [Pubmed]
  9. Postnatal maturation of phosphodiesterase 5 (PDE5) in piglet pulmonary arteries: activity, expression, effects of PDE5 inhibitors, and role of the nitric oxide/cyclic GMP pathway. Moreno, L., Losada, B., Cogolludo, A., Lodi, F., Lugnier, C., Villamor, E., Moro, M., Tamargo, J., Pérez-Vizcaíno, F. Pediatr. Res. (2004) [Pubmed]
  10. Contribution of phosphodiesterase isoenzymes and cyclic nucleotide efflux to the regulation of cyclic GMP levels in aortic smooth muscle cells. Mercapide, J., Santiago, E., Alberdi, E., Martinez-Irujo, J.J. Biochem. Pharmacol. (1999) [Pubmed]
  11. Inhibitory effects of flavonoids on phosphodiesterase isozymes from guinea pig and their structure-activity relationships. Ko, W.C., Shih, C.M., Lai, Y.H., Chen, J.H., Huang, H.L. Biochem. Pharmacol. (2004) [Pubmed]
  12. Stimulation of AQP2 membrane insertion in renal epithelial cells in vitro and in vivo by the cGMP phosphodiesterase inhibitor sildenafil citrate (Viagra). Bouley, R., Pastor-Soler, N., Cohen, O., McLaughlin, M., Breton, S., Brown, D. Am. J. Physiol. Renal Physiol. (2005) [Pubmed]
  13. Bronchial anti-spasmogenic effects and selectivity of T-440, phosphodiesterase type 4 inhibitor, in the dog. Yamagata, S., Wada, K., Sugaya, T., Oka, K., Kaminuma, O., Kikkawa, H., Ikezawa, K. Biol. Pharm. Bull. (1997) [Pubmed]
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