Department of Pharmaceutical Sciences, Tokyo Metropolitan Institute of Public Health , Tokyo, Japan.
Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2020 Dec;37(12):2023-2032. doi: 10.1080/19440049.2020.1826582. Epub 2020 Nov 2.
A compound with potent inhibitory activity for phosphodiesterase type 5 (PDE5) was identified as an illegal adulteration in a libido-boosting dietary supplement being sold at a store in Tokyo. This compound was identified as 5,6-diethyl-2-{5-[(4-methylpiperazin-1-yl)sulphonyl]-2-propoxyphenyl}pyrimidin-4(3)-one using liquid chromatography-diode array detector (LC-DAD), liquid chromatography-tandem mass spectrometer (LC-MS), LC-HRMS, nuclear magnetic resonance (NMR), and X-ray crystallography. The IC value of the inhibitory activity for PDE5A1 (one of the PDE5 isoforms) was 2.0 nM (sildenafil IC value was 4.5 nM). This compound was previously synthesised as a PDE5 inhibitor by Shanghai Institute of Materia Medica. The dietary supplement contained 85 mg of this compound in a capsule, which was about 26% of the capsule content (320 mg).
一种具有强磷酸二酯酶 5（PDE5）抑制活性的化合物被鉴定为一种在东京一家商店销售的壮阳膳食补充剂中的非法掺杂物。该化合物通过液相色谱-二极管阵列检测器（LC-DAD）、液相色谱-串联质谱（LC-MS）、LC-HRMS、核磁共振（NMR）和 X 射线晶体学被鉴定为 5,6-二乙基-2-{5-[(4- 甲基哌嗪-1-基)磺酰基]-2-丙氧基苯基}嘧啶-4(3)-酮。该化合物对 PDE5A1（PDE5 同工酶之一）的抑制活性 IC 值为 2.0 nM（西地那非的 IC 值为 4.5 nM）。该化合物先前由上海药物研究所合成作为 PDE5 抑制剂。膳食补充剂每粒胶囊含有 85 毫克这种化合物，约占胶囊含量的 26%（320 毫克）。
