Tadalafil: Scientific Profile
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Selective inhibitor of long-acting phosphodiesterase-5 (PDE5). Used in research models for the study of vascular hemodynamics and endothelial function in biological systems.
Tadalafil is a compound belonging to the class of selective phosphodiesterase type 5 (PDE5) inhibitors, with a chemical structure derived from the pyrazinopyridoindoles. In scientific research settings, it is distinguished from other PDE5 inhibitors by its extended pharmacokinetic profile, allowing an observation window of up to 36 hours after administration in biological models. This compound acts by inhibiting the degradation of cyclic guanosine monophosphate (cGMP) in vascular smooth muscle cells.
Current research focuses on the role of Tadalafil in the modulation of systemic and pulmonary vascular resistance, as well as on its potential ability to mitigate ischemia-reperfusion damage. Preclinical studies suggest that the PDE5 suppression mediated by this agent may positively influence endothelial integrity and nitric oxide signaling, facilitating the transport of oxygen and nutrients in specific tissues.
Additionally, its application is investigated in models of benign prostatic hypertrophy and in the regulation of pulmonary arterial pressure. Its high selectivity minimizes interaction with PDE6 (present in the retina) compared with other compounds of the same family, which makes it a preferred subject of study for long-duration protocols that evaluate bioavailability and adaptive vascular response.
Mechanism of action
The main mechanism consists of the competitive and selective inhibition of the phosphodiesterase type 5 (PDE5) enzyme. By blocking this enzyme, Tadalafil prevents the hydrolysis of cGMP to 5'-GMP. The intracellular increase in cGMP activates protein kinase G (PKG), which results in a decrease in cytosolic calcium levels and the subsequent relaxation of the smooth muscle in the walls of the blood vessels, promoting vasodilation via the Nitric Oxide/cGMP pathway.
Mechanism summary
It acts through selective inhibition of the enzyme PDE5, increasing intracellular cGMP levels to induce relaxation of vascular smooth muscle.
Clinical Studies (8)
- Tadalafil for the treatment of benign prostatic hyperplasia (Mónica FZ et al. · Expert opinion on pharmacotherapy · 2019) PMID 30901259.
- 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.
- Efficacy and safety of long-term tadalafil 5 mg once daily combined with sildenafil 50 mg as needed at the early stage of treatment for patients with erectile dysfunction (Cui H et al. · Andrologia · 2015) PMID 24387078.
- Randomized Trial of Macitentan/Tadalafil Single-Tablet Combination Therapy for Pulmonary Arterial Hypertension. (Grünig E, et al. · J Am Coll Cardiol · 2024) PMID 38267108.
- Tadalafil therapy for pulmonary arterial hypertension. (Galiè N, et al. · Circulation · 2009) PMID 19470885.
- Initial combination therapy with macitentan and tadalafil in patients with pulmonary arterial hypertension, with and without cardiac comorbidities. (McLaughlin VV, et al. · Eur J Heart Fail · 2024) PMID 38966990.
- Tadalafil for Treatment of Combined Postcapillary and Precapillary Pulmonary Hypertension in Patients With Heart Failure and Preserved Ejection Fraction: A Randomized Controlled Phase 3 Study. (Hoeper MM, et al. · Circulation · 2024) PMID 38939948.
- Tamsulosin plus Tadalafil compared with Tamsulosin alone for benign prostate hyperplasia in patients with or without erectile dysfunction: a meta-analysis and meta-regression of randomized controlled trials. (Hashmi TM, et al. · World J Urol · 2025) PMID 40349279.
Warnings
Tadalafil is a compound exclusively for research use (RUO); the following warnings and handling considerations apply to its use in the laboratory:
- Product exclusively for laboratory research use
- Avoid concurrent administration with nitric oxide donors
- Requires handling under sterile conditions if reconstituted
- Not suitable for use as a supplement or over-the-counter drug
- Study subjects with a history of severe renal insufficiency
- Biological models with pre-existing arterial hypotension
- Coadministration with organic nitrates in any form
- Presence of degenerative alterations of the retina
Technical data
- CAS
- 171596-29-5
- Molecular formula
- C22H19N3O4
- Molecular weight
- 389.4 Da
- Compound type
- metabolic
- Storage
- 20-25°C (Controlled room temperature)
- Shelf life (lyophilized)
- 36 months
- Shelf life (reconstituted)
- Not applicable
- Light-sensitive
- No
Frequently asked questions about Tadalafil
What is Tadalafil?
Selective inhibitor of long-acting phosphodiesterase-5 (PDE5). Used in research models for the study of vascular hemodynamics and endothelial function in biological systems.
What is the mechanism of action of Tadalafil?
It acts through selective inhibition of the enzyme PDE5, increasing intracellular cGMP levels to induce relaxation of vascular smooth muscle.
What is Tadalafil researched for?
In preclinical research, Tadalafil is studied mainly in: Research on the modulation of endothelial function; Study of hemodynamics in the pulmonary vasculature; Evaluation of the reduction of peripheral resistance. Material exclusively for scientific research.
What are the chemical properties of Tadalafil?
Molecular formula C22H19N3O4; molecular weight 389.4 Da; CAS number 171596-29-5.
How is Tadalafil stored?
Storage conditions: 20-25°C (Controlled room temperature); lyophilized stability: 36 months; once reconstituted: Not applicable.
What routes of administration are studied for Tadalafil?
In research models the following are described: Oral. Use is exclusively for scientific research.