Pharmacokinetics of ML3403 ({4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-Type p38 Mitogen-Activated Protein Kinase Inhibitor

No abstract is available for this paper.

• Publication year

  2007

• Venue

  Drug Metabolism And Disposition

• Publication date

  2007-06-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/dmd.106.013409PMID 17344341
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• In vitro metabolite identification of ML3403, a 4-pyridinylimidazole-type p38 MAP kinase inhibitor by LC-Qq-TOF-MS and LC-SPE-cryo-NMR/MS

  2007cited by this paper
• New approaches to the treatment of inflammatory disorders small molecule inhibitors of p38 MAP kinase.

  2006cited by this paper
• Small molecular anti‐cytokine agents

  2006cited by this paper
• Structure elucidation of phase II metabolites by tandem mass spectrometry: an overview.

  2005cited by this paper
• Small molecule p38 inhibitors: novel structural features and advances from 2002-2005.

  2005cited by this paper
• P38 MAP kinase inhibitors: evolution of imidazole-based and pyrido-pyrimidin-2-one lead classes.

  2005cited by this paper
• Modeling Kinetic Data from In Vitro Drug Metabolism Enzyme Experiments

  2004cited by this paper
• Signaling transduction: target in osteoarthritis

  2004cited by this paper
• Inhibitors of p38 Mitogen-Activated Protein Kinase

  2003cited by this paper
• Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes.

  2003cited by this paper
• SB-242235, a selective inhibitor of p38 mitogenactivated protein kinase. I: Preclinical pharmacokinetics

  2002cited by this paper
• SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. II: In vitro and in vivo metabolism studies and pharmacokinetic extrapolation to man

  2002cited by this paper
• Inhibition of stress-activated MAP kinases induces clinical improvement in moderate to severe Crohn's disease.

  2002cited by this paper
• Preclinical pharmacokinetics of SB-203580, a potent inhibitor of p38 mitogen-activated protein kinase

  2001influential reference
• Integrated Cytochrome P450 Reaction Phenotyping: Attempting to Bridge the Gap Between cDNA-expressed Cytochromes P450 and Native Human Liver Microsomes

  1999influential reference
• RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase.

  1999cited by this paper
• Effect of methanol, ethanol, dimethyl sulfoxide, and acetonitrile on in vitro activities of cDNA-expressed human cytochromes P-450.

  1999cited by this paper
• Molecular and physical mechanisms of first-pass extraction.

  1999cited by this paper
• Species and sex differences in expression of flavin-containing monooxygenase form 3 in liver and kidney microsomes.

  1999cited by this paper
• Integrated cytochrome P450 reaction phenotyping: attempting to bridge the gap between cDNA-expressed cytochromes P450 and native human liver microsomes.

  1999cited by this paper
• Effect of common organic solvents on in vitro cytochrome P450-mediated metabolic activities in human liver microsomes.

  1998cited by this paper
• The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data.

  1997cited by this paper
• New drugs for asthma

  1996cited by this paper
• Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance.

  1994cited by this paper
• Physiological Parameters in Laboratory Animals and Humans

  1993cited by this paper
• Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes.

  1992cited by this paper
• Hepatic clearance of drugs. I. Theoretical considerations of a “well-stirred” model and a “parallel tube” model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance

  1977cited by this paper

• p38 mitogen‐activated protein kinase: Functions and targeted therapy in diseases

  2023cites this paper
• Prediction of regioselectivity and preferred order of metabolisms on CYP1A2-mediated reactions. Part 2: Solving substrate interactions of CYP1A2 with non-PAH substrates on the template system.

  2017cites this paper
• 2‐Alkylsulfanyl‐4(5)‐aryl‐5(4)‐heteroarylimidazoles: An Overview on Synthetic Strategies and Biological Activity

  2017cites this paper
• From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors

  2017cites this paper
• Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases.

  2017cites this paper
• Are Two Better Than One in Rheumatoid Arthritis? Development of Dual p38α MAPK/PDE-4 Inhibitors for Treatment of TNFα-Driven Diseases

  2017cites this paper
• The use of in vitro models to study drug permeability and irritancy in the presence of mucus

  2015cites this paper
• Sex-, tissue-, and exposure duration-dependent effects of imidacloprid modulated by piperonyl butoxide and menadione in rats. Part I: oxidative and neurotoxic potentials

  2014cites this paper
• Efficacy and gastrointestinal tolerability of ML3403, a selective inhibitor of p38 MAP kinase and CBS-3595, a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 in CFA-induced arthritis in rats.

  2014cites this paper
• Recent developments of p38α MAP kinase inhibitors as antiinflammatory agents based on the imidazole scaffolds.

  2013cites this paper
• In Vitro Effects of SB202190 on Echinococcus granulosus

  2013cites this paper
• Critical review of p38 MAP kinase inhibitors: a bioanalytical perspective.

  2012cites this paper
• Pharmacophore design of p38α MAP kinase inhibitors with either 2,4,5-trisubstituted or 1,2,4,5-tetrasubstituted imidazole scaffold.

  2011cites this paper
• Chiral sulfoxides as metabolites of 2-thioimidazole-based p38α mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.

  2011cites this paper
• Trisubstituted Purines Are Useful Tools for Developing Potent Plant Mitogen-Activated Protein Kinase Inhibitors

  2010cites this paper
• Novel p38 MAPK inhibitor ML3403 has potent anti-inflammatory activity in airway smooth muscle.

  2010cites this paper
• Colocalization of the VEGF‐R2 and the common IL‐3/GM‐CSF receptor beta chain to lipid rafts leads to enhanced p38 activation

  2009cites this paper
• 2‐Acylaminopyridin‐4‐ylimidazoles as p38 MAP Kinase Inhibitors: Design, Synthesis, and Biological and Metabolic Evaluations

  2009cites this paper
• Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development.

  2009cites this paper
• (cid:1) , (cid:2) -Unsaturated aldehydes contained in cigarette smoke elicit IL-8 release in pulmonary cells through mitogen-activated protein kinases

  2009influential citation
• alpha,beta-Unsaturated aldehydes contained in cigarette smoke elicit IL-8 release in pulmonary cells through mitogen-activated protein kinases.

  2009cites this paper
• Substrate specificity, inhibitors and regulation of human cytochrome P450 2D6 and implications in drug development.

  2009cites this paper
• Characterization and inhibition of a p38-like mitogen-activated protein kinase (MAPK) from Echinococcus multilocularis: antiparasitic activities of p38 MAPK inhibitors.

  2008cites this paper
• Design, synthesis, and biological evaluation of novel Tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzyme's surface-exposed front region.

  2008cites this paper