Determination of a novel low-voltage-activated calcium channel blocker (HYP-10) in rat plasma by liquid chromatography-mass spectrometry

作者:Noh Keumhan; Kim Seo Young; Kam Yoo Lim; Choo Hea Young Park; Lee Hwa Jeong*; Kang Wonku
来源:Journal of Pharmaceutical and Biomedical Analysis, 2011, 54(3): 568-571.
DOI:10.1016/j.jpba.2010.10.007

摘要

A novel T-type calcium channel blocker, 4-amino-1-{4-[(4-chloro-phenyl)-Phenyl-methyl]-piperazin-1-yl}-butan-1-one (HYP-10) has been synthesized, and the compound has shown promise as both a nociceptive and inflammatory pain reliever as well as an analgesic in a rat neuropathic pain model. A quantification method was developed for the determination of HYP-10 in rat plasma. After simple protein precipitation with methanol, HYP-10 and the internal standard, methaqualone were chromatographed on a reversed-phase column and detected by liquid chromatography/tandem mass spectrometry with electrospray ionization. The accuracy and precision of the assay were in accordance with FDA regulations for validation of bioanalytical methods. This method was applied to measure the plasma HYP-10 concentration after a single intravenous administration of the compound in rats.

  • 出版日期2011-2-20