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Rat Pharmacokinetics and In Vitro Metabolite Identification of KM-819, a Parkinson's Disease Candidate, Using LC-MS/MS and LC-HRMS.
Molecules
February 2024
Graduate School of New Drug Discovery and Development, Chungnam National University, Daejeon 34134, Republic of Korea.
Article Synopsis
- - FAF1 is a protein linked to cell death mechanisms and is overexpressed in dopaminergic neurons in patients with Parkinson's disease; KM-819, an FAF1 inhibitor, shows promise in protecting these neurons and reducing harmful protein levels.
- - A quantitative method for measuring KM-819 in rat plasma was developed using liquid chromatography-tandem mass spectrometry, achieving good precision and accuracy within a specific concentration range.
- - The method confirmed KM-819's stability under various conditions and met regulatory standards, enabling successful application in pharmacokinetic studies in rats.
Preclinical PK investigation of a novel IDO1/TDO dual inhibitor-SHR9146 in mouse plasma and tissues by LC-MS/MS.
Front Oncol
July 2023
Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
Purpose: The aim of the present study was to establish a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of SHR9146, a novel IDO1/TDO dual inhibitor, in mouse plasma and tissues, and to apply it to investigate the preclinical plasma pharmacokinetics and tissue distribution of SHR9146 in mice.
Methods: Samples were spiked with deuterated SHR9146-d as an internal standard and pretreated by protein-precipitation extraction with methanol. Chromatographic separation was performed on a Venusil ABS C18 column (150 × 4.
ATP modulates self-perpetuating conformational conversion generating structurally distinct yeast prion amyloids that limit autocatalytic amplification.
J Biol Chem
May 2023
Centre for Protein Science, Design and Engineering, Indian Institute of Science Education and Research (IISER) Mohali, Punjab, India; Department of Biological Sciences, Indian Institute of Science Education and Research (IISER) Mohali, Punjab, India; Department of Chemical Sciences, Indian Institute of Science Education and Research (IISER) Mohali, Punjab, India. Electronic address:
Prion-like self-perpetuating conformational conversion of proteins into amyloid aggregates is associated with both transmissible neurodegenerative diseases and non-Mendelian inheritance. The cellular energy currency ATP is known to indirectly regulate the formation, dissolution, or transmission of amyloid-like aggregates by providing energy to the molecular chaperones that maintain protein homeostasis. In this work, we demonstrate that ATP molecules, independent of any chaperones, modulate the formation and dissolution of amyloids from a yeast prion domain (NM domain of Saccharomyces cerevisiae Sup35) and restricts autocatalytic amplification by controlling the amount of fragmentable and seeding-competent aggregates.
View Article and Find Full Text PDFPreclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration.
Molecules
June 2022
School of Pharmacy, Nantong University, Nantong 226001, China.
Oxypeucedanin, a furanocoumarin extracted from many traditional Chinese herbal medicines, has a variety of pharmacological effects. However, the independent pharmacokinetic characteristics and bioavailability of this compound remains elusive. In this study, a rapid, sensitive, and selective method using ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC/MS/MS) was developed for evaluating the intravenous and oral pharmacokinetics of oxypeucedanin.
View Article and Find Full Text PDF[C]mHED PET follows a two-tissue compartment model in mouse myocardium with norepinephrine transporter (NET)-dependent uptake, while [F]LMI1195 uptake is NET-independent.
EJNMMI Res
September 2020
Department of Nuclear Medicine, University Hospital Zurich, Raemistrasse 100, 8091, Zurich, Switzerland.
Purpose: Clinical positron emission tomography (PET) imaging of the presynaptic norepinephrine transporter (NET) function provides valuable diagnostic information on sympathetic outflow and neuronal status. As data on the NET-targeting PET tracers [C]meta-hydroxyephedrine ([C]mHED) and [F]LMI1195 ([F]flubrobenguane) in murine experimental models are scarce or lacking, we performed a detailed characterization of their myocardial uptake pattern and investigated [C]mHED uptake by kinetic modelling.
Methods: [C]mHED and [F]LMI1195 accumulation in the heart was studied by PET/CT in FVB/N mice.
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