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The importance of research and development in science can not be over-emphasized. It is paramount to have a trustworthy supplier of research liquids. Loti Labs is a leader in the research industry. We have in stock a variety of high-quality research chemicals used for scientific research. The one we will be discussing in this article is the research chemical Tadalafil. It is available for sale for research purposes only and not for human consumption.

WHAT IS TADALAFIL CITRATE

Tadalafil is a selective inhibitor of the enzyme phosphodiesterase type 5

(PDE5), identified in the smooth muscle cells of the corpus cavernosum, vascular and visceral smooth muscle, skeletal muscle, platelets, kidney, lung, cerebellum, prostate, urethra, and bladder. It is one of a family of 11 PDEs that degrade cyclic guanosine monophosphate

or cyclic adenosine monophosphate, or both.

Its empirical formula is C₂₂O₄H₁₉N₃, with a molecular weight of 389.41g/mol. Tadalafil has a unique structure.

Scientific data suggest that inhibition of PDE-5 may improve signs and symptoms of Erectile Dysfunction, Benign Prostatic Hyperplasia, and other Lower Urinary Tract Symptoms through relaxation of smooth muscle and reduction in endothelial cell proliferation in the prostate, bladder, and pelvic vasculature leading to increased perfusion of the lower urinary tract.

STRUCTURE OF TADALAFIL

IUPAC name: 2R,8R)-2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione

Molecular Formula: C₂₂O₄H₁₉N₃

Molecular weight:389.4 g/mol

CAS number: 171596-29-5

MECHANISM OF ACTION

The mechanism of Tadalafil for improved Lower Urinary Tract Symptoms is thought to be related to three principal theories:

1. Alterations in nitric oxide levels
2. Inhibition of Phosphodiesterase-5
3. Reductions in pelvic atherosclerosis

PDE5 catalyzes the breakdown of the potent smooth muscle-relaxing agent cyclic guanosine monophosphate (cGMP), a second messenger of nitric oxide. The inhibition of PDE5 increases cGMP levels, reduces intracellular calcium and induces vasodilation.

It is rapidly absorbed after oral administration with an onset time of 30-120mins post-dose. Only about 36% of the dose is absorbed from an oral solution.

TADALAFIL EFFECTS

The wide range of benefits that tadalafil exerts is as a result of its multifactorial mechanism of actions on various organs in animal test subjects. Its effects include the following:

• It improves erectile dysfunction in research subjects that is defined as not attaining and maintaining a penile erection that is sufficient for satisfactory sexual performance. Nitric oxide’s release triggers the production of cyclic guanosine monophosphate (cGMP), relaxing the corpora cavernosa in an erection. Tadalafil enhances erection by inhibiting phosphodiesterase-5 preventing the breakdown of cyclic guanosine monophosphate.

• It improves depression and cognitive functions in experimental animals with inflammatory, neurodegenerative, and memory loss diseases like Alzheimer’s disease.

• It prevents the formation of urethral strictures after a urethral injury in animal test subjects by inhibiting the phosphodiesterase-5 pathway.

• It reduces inflammation in endothelial cells of pulmonary arteries in rats reducing the effects of pulmonary arterial hypertension.

• It relaxes vascular smooth muscle, increases blood perfusion and oxygenation of the prostatic tissue of animal test subjects, restoring the tissue structure in the prostate. This improves the storage and voiding of urinary symptoms observed in lower urinary tract diseases and benign prostatic hyperplasia.

• It demonstrates cardio-protection in experimental myocardial infarction by inhibiting the PDE-5 found in smooth muscle cells of arteries, and veins substantially reducing ischemic cell death.

• It facilitates fetal growth in animal test subjects with L-NG-nitroarginine methyl ester (L-NAME)-induced preeclampsia (PE) with fetal growth restriction (FGR) by dilating the maternal blood sinuses in the placenta, encouraging the growth of the fetus.

LOOKING FOR WHERE TO BUY RESEARCH LIQUIDS

Tadalafil can be purchased from Loti Labs. It is important to buy research fluids which are USA-made to ensure the integrity of your research. Tadalafil sold from Loti Labs is tested to ensure quality. Tadalafil is commonly sold in 30mg per ml vials. It is available in liquid form.

References:

1. National Center for Biotechnology Information. PubChem Database. Tadalafil, CID=110635, https://pubchem.ncbi.nlm.nih.gov/compound/Tadalafil (accessed on Dec. 7, 2019)

1. Washington SL 3rd, Shindel AW. A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy. Drug Des Devel Ther. 2010;4:159–171. Published 2010 Sep 7. doi:10.2147/dddt.s9067

1. Urios, A., Ordoño, F., García-García, R. et al. Tadalafil Treatment Improves Inflammation, Cognitive Function, And Mismatch Negativity Of Patients With Low Urinary Tract Symptoms And Erectile Dysfunction. Sci Rep 9, 17119 (2019) doi:10.1038/s41598-019-53136-y

1. Sesti, C., Florio, V., Johnson, E. et al. The phosphodiesterase-5 inhibitor tadalafil reduces myocardial infarct size. Int J Impot Res 19, 55–61 (2007) doi:10.1038/sj.ijir.3901497

1. Seftel, A., Farber, J., Fletcher, J. et al. A three-part study to investigate the incidence and potential etiologies of tadalafil-associated back pain or myalgia. Int J Impot Res 17, 455–461 (2005) doi:10.1038/sj.ijir.3901374

1. Tachibana, R., Umekawa, T., Yoshikawa, K. et al. Tadalafil treatment in mice for preeclampsia with fetal growth restriction has neuro-benefic effects in offspring through modulating prenatal hypoxic conditions. Sci Rep 9, 234 (2019) doi:10.1038/s41598-018-36084-x

1. Gong, Y., Xu, C., Wang, J. et al. Inhibition of phosphodiesterase 5 reduces bone mass by suppression of canonical Wnt signaling. Cell Death Dis 5, e1544 (2014) doi:10.1038/cddis.2014.510