MEGATON, a dietary supplement, was analyzed in order to detect PDE-5 inhibitors and their analogues. A new analogue of vardenafil could be detected by high-performance liquid chromatography (HPLC) analysis with a photodiode array detector (PDA). This compound was compared with sildenafil, tadalafil, and vardenafil as well as their structurally modified analogues such as hongdenafil and homosildenafil. The structure of this compound was elucidated by mass spectrometry (MS), infrared (IR) spectroscopy and one- and two-dimensional nuclear magnetic resonance (NMR) spectroscopy. When compared with vardenafil to verify the structural difference, this compound had an acetyl group instead of a sulfonyl group in the pyrazolopyrimidine portion without any substitution in the piperazine ring of the molecule. This compound was identified as 2-(2-ethoxy-5-(2-(4-ethylpiperazin-1-yl)acetyl)phenyl)-5-methyl-7-propyl-imidazo(5,1-f)-(1,2,4)triazin-4(3H)-one, which is also called acetylvardenafil.
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http://dx.doi.org/10.1016/j.jpba.2010.09.022 | DOI Listing |
J Pharm Biomed Anal
January 2025
Division of Research and Analysis, Taiwan Food and Drug Administration, No.161-2 Kunyang St., Nangang District, Taipei City 115-61, Taiwan, ROC. Electronic address:
Food Addit Contam Part A Chem Anal Control Expo Risk Assess
December 2023
Laboratoire SPCMIB (UMR CNRS 5068), Université Paul Sabatier, Université de Toulouse, Toulouse cedex, France.
This article is an up-to-date review of 112 unapproved phosphodiesterase type 5 inhibitors (PDE-5i) found as adulterants in sexual enhancement dietary supplements and other products from 2003 to July 2023. Seventy-five of these unapproved PDE-5i are analogues of sildenafil (67%), followed by 26 analogues of tadalafil (23%), 9 analogues of vardenafil (8%) and 2 other type of compounds (2%). The products have been formulated in various packaging, primarily in capsule, tablet, and powder forms.
View Article and Find Full Text PDFCochrane Database Syst Rev
November 2023
Department of Medicine and Epidemiology and Biostatistics, University of Western Ontario, London, Canada.
Background: Raynaud's phenomenon is a vasodilatory phenomenon characterised by digital pallor, cyanosis, and pain of the extremities. Primary Raynaud's phenomenon has no underlying disease associated with it, while secondary Raynaud's phenomenon is associated with connective tissue disorders such as systemic sclerosis. Systemic sclerosis causes fibrosis and commonly affects the skin and internal organs such as the gastrointestinal tract, lungs, kidney, and heart.
View Article and Find Full Text PDFObjective: This study is aimed to develop a qualitative and quantitative method to detect a novel vardenafil analogue from a healthcare product, which is claimed to enhance sexual function. The unknown compound was detected by non-targeted screening using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF-MS). MS spectra showed that the characteristic fragment ions of this unknown compound were highly similar to those of vardenafil.
View Article and Find Full Text PDFTalanta
January 2024
Bilecik Seyh Edebali University, Bioengineering Department, Bilecik, Turkey. Electronic address:
Tadalafil is one of the selective phosphodiesterase type 5 inhibitors (PDE5) and serves as the active compound in drugs used for the treatment of erectile dysfunction. These PDE5 inhibitors are prescribed under medical supervision. However, cases of adulteration of dietary supplements with PDE5 inhibitors or their unapproved analogs have been reported worldwide.
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