Results 11 to 20 of about 27,101 (273)

In vitro metabolism, reaction phenotyping, enzyme kinetics, CYP inhibition and induction potential of ataluren

Pharmacology Research & Perspectives, 2020
Ataluren promotes ribosomal readthrough of premature termination codons in mRNA which result from nonsense mutations. In vitro studies were performed to characterize the metabolism and enzyme kinetics of ataluren and its interaction potential with CYP ...
Ronald Kong, Jiyuan Ma, Seongwoo Hwang, Young‐Choon Moon, Ellen M. Welch, Marla Weetall, Joseph M. Colacino, Neil Almstead, John Babiak, Elizabeth Goodwin   +9 more
doaj   +1 more source

Study on In Vitro Metabolism and In Vivo Pharmacokinetics of Beauvericin

Toxins, 2022
Beauvericin (BEA) is a well-known mycotoxin produced by many fungi, including Beaveria bassiana. The purpose of this study was to evaluate the in vitro distribution and metabolism characteristics as well as the in vivo pharmacokinetic (PK) profile of BEA.
Yu Yuan, Guangpeng Meng, Yuanbo Li, Chunjie Wu   +3 more
doaj   +1 more source

Studies on the inhibitory effect of isavuconazole on flumatinib metabolism in vitro and in vivo

Frontiers in Pharmacology, 2023
As the validated agent for the treatment of chronic myelogenous leukemia (CML), flumatinib is a novel oral tyrosine kinase inhibitor (TKI) with higher potency and selectivity for BCR-ABL1 kinase compared to imatinib.
Ya-nan Liu, Ya-nan Liu, Xinhao Xu, Xinhao Xu, Jingjing Nie, Jingjing Nie, Yingying Hu, Xuegu Xu, Ren-ai Xu, Xiaoxiang Du   +9 more
doaj   +1 more source

Biotransformation of (−)-Verbenone by Human Liver Microsomes

Bioscience, Biotechnology, and Biochemistry, 2002
The biotransformation of (-)-verbenone was investigated with human liver microsomes by using GC-MS. Regioselective biotransformation was observed when (-)-verbenone was incubated with the liver microsomes. (-)-10-Hydroxyverbenone was formed from (-)-verbenone of kinetic analysis showed that the Km and Vmax values for the hydroxylation of (-)-verbenone ...
MIYAZAWA, Mitsuo, SUGIE, Atsushi, SHINDO, Masaki   +2 more
openaire   +2 more sources

Morphine Metabolism in Human Skin Microsomes [PDF]

, 2012
For patients with severe skin wounds, topically applied morphine is an option to induce efficient analgesia due to the presence of opioid receptors in the skin.
Heilmann, S., Küchler, S., Schäfer-Korting, Monika, Küchler, Sarah, Schäfer-Korting, M.   +4 more
core   +1 more source

Nontargeted Metabolomics by High-Resolution Mass Spectrometry to Study the In Vitro Metabolism of a Dual Inverse Agonist of Estrogen-Related Receptors β and γ, DN203368

Pharmaceutics, 2021
DN203368 ((E)-3-[1-(4-[4-isopropylpiperazine-1-yl]phenyl) 3-methyl-2-phenylbut-1-en-1-yl] phenol) is a 4-hydroxy tamoxifen analog that is a dual inverse agonist of estrogen-related receptor β/γ (ERRβ/γ).
Sin-Eun Kim, Seung-Bae Ji, Euihyeon Kim, Minseon Jeong, Jina Kim, Gyung-Min Lee, Hyung-Ju Seo, Subin Bae, Yeojin Jeong, Sangkyu Lee, Sunghwan Kim, Taeho Lee, Sung Jin Cho, Kwang-Hyeon Liu   +13 more
doaj   +1 more source

3-hydroxy-3-methylglutaryl coenzyme A reductase in human liver microsomes: active and inactive forms and cross-reactivity with antibody against rat liver enzyme.

Journal of Lipid Research, 1984
3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme catalyzing the rate-limiting step in cholesterol biosynthesis, exists in one active (dephosphorylated) and one inactive (phosphorylated) form in liver microsomes obtained from several ...
B Angelin, K Einarsson, L Liljeqvist, K Nilsell, RA Heller   +4 more
doaj   +1 more source

Identification and interspecies characterization of UDP-glucuronosyltransferase isoforms catalyzing acacetin glucuronidation using recombinant UGT enzymes and microsomes

Journal of Traditional Chinese Medical Sciences, 2019
Objective: To explore the glucuronic acid metabolism of acacetin in human liver and intestinal microsomes to better characterize human uridine 5′-diphospho (UDP)-glucuronosyltransferase (UGT) isoforms. In addition, interspecies comparisons were performed
Kangle Shi, Shan Li, Qinggang Meng
doaj   +1 more source

Characterisation of theophylline metabolism by human liver microsomes [PDF]

Biochemical Pharmacology, 1987
1. A radiometric high performance liquid chromatographic method is described for the assay of theophylline metabolism in vitro by the microsomal fraction of human liver. 2. Formation of the three metabolites of theophylline (3‐methylxanthine, 1‐methylxanthine and 1,3‐ dimethyluric acid) were linear with protein concentrations to 4 mg ml‐1 and with ...
R A, Robson, A P, Matthews, J O, Miners, M E, McManus, U A, Meyer, P M, Hall, D J, Birkett   +6 more
openaire   +2 more sources

In vitro modulatory effects of Terminalia arjuna, arjunic acid, arjunetin and arjungenin on CYP3A4, CYP2D6 and CYP2C9 enzyme activity in human liver microsomes

Toxicology Reports, 2015
Terminalia arjuna is a tree having an extensive medicinal potential in cardiovascular disorders. Triterpenoids are mainly responsible for cardiovascular properties. Alcoholic and aqueous bark extracts of T.
Alice Varghese, Jay Savai, Nancy Pandita, Ram Gaud   +3 more
doaj   +1 more source