Sildenafil: Scientific Profile
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Selective inhibitor of phosphodiesterase type 5 (PDE5) used in research for the study of hemodynamic dynamics and the relaxation of vascular smooth muscle via the cGMP pathway.
Sildenafil is a chemically synthesized compound belonging to the class of selective phosphodiesterase inhibitors, specifically designed to modulate the enzymatic degradation of cyclic guanosine monophosphate (cGMP) in the corpora cavernosa and the pulmonary vasculature. In research settings, its main application lies in the observation of vascular smooth muscle dilation, mediated by the release of nitric oxide and the subsequent accumulation of cGMP secondary to the enzymatic inhibition of PDE5.
Experimental models have used this compound to analyze its impact on pulmonary hypertension and endothelial dysfunction, providing data on systemic vascular resistance and peripheral blood flow. By acting on the nitric oxide signaling cascade, Sildenafil allows researchers to evaluate the responsiveness of smooth tissues to controlled vasodilatory stimuli.
In addition to its hemodynamic effects, Sildenafil has been the subject of study in neurology and experimental oncology protocols to evaluate its potential in blood-brain barrier permeability and the modulation of chronic inflammatory responses. Its pharmacokinetic profile in research subjects demonstrates constant absorption, which facilitates replicability in dose-response studies within vascular physiology laboratories.
Mechanism of action
It acts through the competitive and selective inhibition of the enzyme phosphodiesterase type 5 (PDE5), which is responsible for the degradation of cGMP in smooth muscle cells. By blocking this enzyme, Sildenafil potentiates intracellular cGMP levels, which results in a prolongation of nitric oxide-mediated relaxation and an increase in tissue blood flow in areas with high expression of PDE5 receptors.
Mechanism summary
PDE5 inhibitor that increases intracellular cGMP levels, promoting smooth muscle relaxation and vasodilation through the nitric oxide pathway.
Clinical Studies (8)
- Sildenafil in Combination Therapy against Cancer: A Literature Review (Iratni R et al. · Current medicinal chemistry · 2021) PMID 32744956.
- Sildenafil/Viagra in the treatment of premature ejaculation (Krishnappa P et al. · International journal of impotence research · 2019) PMID 30837718.
- Direct comparison of tadalafil with sildenafil for the treatment of erectile dysfunction: a systematic review and meta-analysis (Gong B et al. · International urology and nephrology · 2017) PMID 28741090.
- Intrapartum Sildenafil to Improve Perinatal Outcomes: A Randomized Clinical Trial. (Kumar S, et al. · JAMA · 2025) PMID 40489090.
- Sildenafil improves clinical signs and radiographic features in dogs with congenital idiopathic megaoesophagus: a randomised controlled trial. (Quintavalla F, et al. · Vet Rec · 2017) PMID 28188161.
- Oral sildenafil versus bosentan for treatment of persistent pulmonary hypertension of the newborn: a randomized controlled trial. (Kallimath A, et al. · BMC Pediatr · 2024) PMID 39487423.
- Cerebrovascular Effects of Sildenafil in Small Vessel Disease: The OxHARP Trial. (Webb AJS, et al. · Circ Res · 2024) PMID 38832504.
- Sildenafil for adult Asian patients with pulmonary arterial hypertension: a systematic review and meta-analysis. (Shi Q, et al. · Ann Palliat Med · 2022) PMID 35144425.
Warnings
Sildenafil is a compound exclusively for research use (RUO); the following warnings and handling considerations apply to its use in the laboratory:
- Exclusive use in laboratory research settings
- Risk of lethal interaction with nitric oxide donors
- Must be stored away from direct light
- Requires dose adjustment in models with hepatic dysfunction
- Concurrent use with organic nitrates
- Models with a history of ischemic optic neuropathy
- End-stage renal failure in study specimens
- Combination with potent CYP3A4 inhibitors without adjustment
Technical data
- CAS
- 139755-83-2
- Molecular formula
- C22H30N6O4S
- Molecular weight
- 474.58 Da
- Compound type
- metabolic
- Storage
- 15-30°C in a dry environment
- Shelf life (lyophilized)
- 36 months
- Shelf life (reconstituted)
- Not applicable
- Light-sensitive
- No
Frequently asked questions about Sildenafil
What is Sildenafil?
Selective inhibitor of phosphodiesterase type 5 (PDE5) used in research for the study of hemodynamic dynamics and the relaxation of vascular smooth muscle via the cGMP pathway.
What is the mechanism of action of Sildenafil?
PDE5 inhibitor that increases intracellular cGMP levels, promoting smooth muscle relaxation and vasodilation through the nitric oxide pathway.
What is Sildenafil researched for?
In preclinical research, Sildenafil is studied mainly in: Modulation of endothelial function in research; Study of peripheral and pulmonary vasodilation; Research on intracellular cGMP signaling. Material exclusively for scientific research.
What are the chemical properties of Sildenafil?
Molecular formula C22H30N6O4S; molecular weight 474.58 Da; CAS number 139755-83-2.
How is Sildenafil stored?
Storage conditions: 15-30°C in a dry environment; lyophilized stability: 36 months; once reconstituted: Not applicable.
What routes of administration are studied for Sildenafil?
In research models the following are described: Oral. Use is exclusively for scientific research.