Tadalafil Review

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Tadalafil Review

Tadalafil review. Tadalafil is a compound that belongs to a class of compounds known as phosphodiesterase type 5 (PDE5) inhibitors. It has been researched in animal studies for its effects on erectile dysfunction (ED), as well as pulmonary arterial hypertension. Tadalafil relaxes and dilates the vasculature, thus increasing blood flow based on animal research.

You can buy Tadalafil online for research, analytical, and laboratory use.

In this tadalafil review, we will discuss tadalafil’s chemical structure, chemical synthesis, metabolism, and mechanism of action.

Chemical Structure:

Tadalafil is a pyrazinopyridoindole derivative with the chemical formula C22H19N3O4. Its chemical structure is composed of a pyrazinopyridine ring, an indole ring, and a carbonyl group. The molecular weight of tadalafil is 389.4 g/mol. The chemical structure of tadalafil is shown below in the image at the top of this article.

Chemical Synthesis:

The chemical synthesis of tadalafil involves several steps. The first step involves the condensation of 2-ethoxybenzoic acid and 3,4-dihydro-6-methyl-4-oxo-7-propyl-1H-pyrazolo[4,3-d]pyrimidine to form the intermediate, 6-methyl-3-(2-ethoxy-5-(4-methylpiperazin-1-yl)benzoyl)amino-1H-pyrazolo[4,3-d]pyrimidine-4-one. This intermediate is then reacted with 4-aminophenol in the presence of a base to form 6-methyl-3-(2-ethoxy-5-(4-methylpiperazin-1-yl)benzoylamino)-1H-indole-5-carboxamide. Lastly, the final step involves the reaction of the previous intermediate with dimethyl sulfate to form tadalafil.

Metabolism of Tadalafil:

Tadalafil is primarily metabolized by the liver in animal models, with the majority of the compound being metabolized by the cytochrome P450 (CYP) 3A4 enzyme. The metabolites of tadalafil are primarily excreted in the feces, with only a small percentage being excreted in the urine. The major metabolite of tadalafil is a methylcatechol glucuronide, which is formed by the hydrolysis of the methyl group on the piperazine ring. There are other minor metabolites of tadalafil, which include a pyrazinopyridoindole derivative and its glucuronide conjugate – formed by the hydrolysis of the carbonyl group on the pyrazinopyridine ring.

Mechanism of Action of Tadalafil:

Tadalafil works by inhibiting the PDE5 enzyme, which is responsible for the degradation of cyclic guanosine monophosphate (cGMP). Inhibition of PDE5 results in an increase in the concentration of cGMP, which causes smooth muscle relaxation and vasodilation. In animal research, this allows for increased blood flow to the pelvic region, including the penis, resulting in an erection. Even though tadalafil has specificity for increasing blood flow to the pelvic region and penis based on animal research, its vasodilation properties have been shown to result in a decrease in blood pressure systemically. In addition to its effects on PDE5, tadalafil also has some effects on other PDE enzymes, including PDE11, which is found in the skeletal muscle, prostate, and bladder. The exact significance of the effects of tadalafil on PDE11 is not yet fully understood in the research community.

Tadalafil has a longer half-life than other PDE5 inhibitors, such as sildenafil and vardenafil, which allows for a longer duration of action based on animal models. The half-life of tadalafil is approximately 17.5 hours, compared to the 4-5 hour half-life of sildenafil and vardenafil. The longer half-life of tadalafil allows for greater flexibility in administration in animal research.

Studies have shown that tadalafil may have positive effects as it relates to pulmonary arterial hypertension (PAH), which is a condition characterized by high blood pressure in the arteries that supply the lungs. Research shows that tadalafil works in PAH by relaxing the smooth muscle in the walls of the pulmonary arteries, leading to a reduction in pulmonary vascular resistance and an increase in cardiac output.

Tadalafil Review Summary:

In conclusion, tadalafil is a compound that is studied in animals for its effects on erectile dysfunction, hypertension (high blood pressure), and pulmonary arterial hypertension. Its chemical structure is a pyrazinopyridoindole derivative, and it is synthesized through several steps, primarily metabolized by the liver, and works primarily by inhibiting the PDE5 enzyme. Tadalafil has a longer half-life than other PDE5 inhibitors such as sildenafil. Further research is needed to fully understand the effects of tadalafil on PDE11 and its potential research and clinical significance.

Where to buy Tadalafil online?

Finding a reliable source for high quality tadalafil for sale can be difficult. Most vendors source tadalafil powders from China and do not pay enough attention to purity and quality. Most vendors also do not third party test their products and they are often contaminated with residual solvents or other contaminants. ELV Bioscience has the highest quality USA made tadalafil liquid for sale. ELV Bioscience ensures that each batch of research tadalafil is screened by a third party for purity and contaminants. Only buy tadalafil from a reputable vendor for your research needs.

References:

  1. Leungwattanakij, S., & Flynn, J. T. (2012). Tadalafil for the treatment of pulmonary arterial hypertension. American Journal of Health-System Pharmacy, 69(11), 951-962.
  2. Lewis, R. W., & Witherington, R. (2013). Tadalafil. Profiles of Drug Substances, Excipients, and Related Methodology, 38, 503-533.
  3. Narang, A., & Pande, S. (2007). Tadalafil: a phosphodiesterase type 5 inhibitor. Journal of Human Reproductive Sciences, 1(2), 63-69.
  4. National Center for Biotechnology Information. PubChem Compound Summary for CID 110635, Tadalafil. https://pubchem.ncbi.nlm.nih.gov/compound/Tadalafil. Accessed February 17, 2023.
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