Quantification of a novel PPARγ partial agonist (S)-2-ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) in rat plasma using liquid chromatography-tandem mass spectrometry

  title={Quantification of a novel PPAR$\gamma$ partial agonist (S)-2-ethoxy-3-(4-\{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy\}-phenyl)-propionic acid (PAM-1616) in rat plasma using liquid chromatography-tandem mass spectrometry},
  author={Hye Won Chae and Hae-Ni Jung and Eun jung Kim and Hyun Joo Shim and Joong Inn Lim and Hye Young Ji and Hye Suk Lee},
  journal={Archives of Pharmacal Research},
Abstract(S)-2-ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) is a novel peroxisome proliferators-activated receptor γ (PPARγ) partial agonist with excellent antihyperglycemic activity. It is a promising new drug candidate for the treatment of type-2 diabetes with reduced possibility of edema in vitro/in vivo. In order to evaluate the pharmacokinetics of PAM-1616, a reliable, selective and sensitive highperformance liquid… 
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Metabolism of a new P-glycoprotein inhibitor HM-30181 in rats using liquid chromatography/electrospray mass spectrometry.
The in vitro and in vivo metabolic pathway of HM-30181 in rats was identified on the basis of liquid chromatography/tandem mass spectrometry (LC/MS/MS) analysis with the synthesized authentic standards.
Liquid chromatography-tandem mass spectrometry of a new PPARα/γ dual agonist PAR-5359 in rat plasma
A reliable, selective and sensitive high-performance liquid chromatography with electrospray ionization tandem mass spectrometry was developed for the determination of PAR-5359 in rat plasma and was successfully applied to the pharmacokinetic study of PAR -5359 after oral dose at a dose of 1 mg/kg to male SD rats.
Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator.
It is established that novel selective PPARgamma modulators can produce altered receptor conformational stability leading to distinctive gene expression profiles, reduced adipogenic cellular effects, and potentially improved in vivo biological responses.
Determination of a Novel Antiangiogenic Agent KR‐31831 in Rat Plasma by Liquid Chromatography‐Tandem Mass Spectrometry
ABSTRACT A liquid chromatography‐tandem mass spectrometric (LC/MS/MS) method was developed for the determination of a new anti‐angiogenic drug KR‐31831 in rat plasma. KR‐31831 and internal standard,
PPAR(gamma) and glucose homeostasis.
Findings suggest that modulation of PPARgamma activity by partial agonists or compounds that affect cofactor recruitment might hold promise for the treatment of insulin resistance.
HPLC-MS/MS in drug metabolism and pharmacokinetic screening.
  • Y. Hsieh
  • Chemistry, Biology
    Expert opinion on drug metabolism & toxicology
  • 2008
This review summarizes high performance liquid chromatography coupled to a tandem mass spectrometer (HPLC-MS/MS) methodologies that are employed in drug metabolism and pharmacokinetic screens for a series of new chemical entities.
PPARs: therapeutic targets for metabolic disease.
Principles and applications of LC-MS in new drug discovery.
The metabolic syndrome: peroxisome proliferator-activated receptor gamma and its therapeutic modulation.
The consequences of inherited variation in the human peroxisome proliferator-activated receptor gamma gene are focused on, linking this receptor to disordered glucose homeostasis, adipogenesis, lipid metabolism, and blood pressure regulation.