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

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 quantif...

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Bibliographic Details
Published in:Journal of pharmaceutical and biomedical analysis 2011-02, Vol.54 (3), p.568-571
Main Authors: Noh, Keumhan, Kim, Seo Young, Kam, Yoo Lim, Choo, Hea-Young Park, Lee, Hwa Jeong, Kang, Wonku
Format: Article
Language:English
Subjects:
Analgesics
Analysis
Analytical, structural and metabolic biochemistry
Animal models
Animals
Biological and medical sciences
Butanones - blood
Butanones - chemistry
Butanones - pharmacokinetics
Butanones - pharmacology
Calcium Channel Blockers - blood
Calcium Channel Blockers - pharmacokinetics
Calcium Channel Blockers - toxicity
Calcium channels
Calcium channels (T-type)
Calcium Channels, T-Type - metabolism
Chromatography, Liquid
Drug Stability
electrospray ionization mass spectrometry
Fundamental and applied biological sciences. Psychology
General pharmacology
HYP-10
Inflammation
Injections, Intravenous
Intravenous administration
intravenous injection
Ionization
LC–MS/MS
Liquid chromatography
LITAF protein
Male
Mass Spectrometry
Mass spectroscopy
Medical sciences
Methanol
Neuralgia - drug therapy
Neuropathy
Novel T-type calcium channel blocker
pain
Pain perception
Pharmacology. Drug treatments
Piperazines - blood
Piperazines - chemistry
Piperazines - pharmacokinetics
Piperazines - pharmacology
Proteins
Rat plasma
Rats
Reproducibility of Results
Spectrometry
Spectrometry, Mass, Electrospray Ionization
tandem mass spectrometry
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Summary: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.
ISSN:0731-7085
1873-264X
DOI:10.1016/j.jpba.2010.10.007