Keywords: متابولیت واکنش پذیر; Benzbromarone; Reactive metabolite; Glutathione adduct; Drug-induced liver injury; CYP; ABT; 1-aminobenzotriazole; BBR; benzbromarone; BSO; l-buthionine-sulfoximine; CYP; cytochrome P450; GSH; glutathione; HLM; human liver microsomes; HPLC; high-performan
مقالات ISI متابولیت واکنش پذیر (ترجمه نشده)
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Keywords: متابولیت واکنش پذیر; Hormone sensitive lipase; Dyslipidemia; Lipolysis; Boronic acid; Reactive metabolite;
Keywords: متابولیت واکنش پذیر; Acyl glucuronide; Drug development; Drug toxicity; In vitro screening; In vivo model; Immune activation; Protein adduct; Reactive metabolite; UDP-glucuronosyltransferase; ADR; adverse drug reaction; AG; acyl glucuronide; AGE; advanced glycation end prod
Keywords: متابولیت واکنش پذیر; AcHz; acetylhydrazine; AcINH; acetylisoniazid; ALP; alkaline phosphatase; ALT; alanine aminotransferase; DiAcHz; diacetylhydrazine; GSH; glutathione; GST; glutathione S-transferase; Hz; hydrazine; INA; isonicotinic acid; INH; isoniazid; MPO; myeloperoxida
Keywords: متابولیت واکنش پذیر; GSH; glutathione; LC/MS; liquid chromatography/mass spectrometry; MRM; multiple reaction monitoring; HRMS; high resolution mass spectrometry; Qtrap; triple quadrupole linear ion trap; EMS; enhanced MS; NL; neutral loss scan; PI; precursor ion scan; MIM; m
Keywords: متابولیت واکنش پذیر; Bioactivation; Biotransformation; Cytochrome P450; Drug development; Drug discovery; Drug metabolism; Electrochemical generation; Electrochemistry; Metabolite synthesis; Reactive metabolite
Keywords: متابولیت واکنش پذیر; Metabolic activation; Reactive metabolite; Cytochrome P450; Drug-induced toxicity; Structural alerts
Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK)
Keywords: متابولیت واکنش پذیر; Bruton's tyrosine kinase; BTK; Reactive metabolite; Covalent binding; Glutathione adduct;
Metabolic-induced cytotoxicity of diosbulbin B in CYP3A4-expressing cells
Keywords: متابولیت واکنش پذیر; AP; Acetaminophen; CCK; 2H-Tetrazolium,5-(2,4-disulfophenyl)-3-(2-methoxy-4-nitrophenyl)-2-(4-nitrophenyl)-,innersalt,sodium salt; CYP450; Cytochrome P450; DB; Diosbulbin B; DMEM; Dulbecco's Modified Eagle Medium; DMF; N,N-Dimethylformamide; DMSO; D
Combined administration of silymarin and vitamin C stalls acetaminophen-mediated hepatic oxidative insults in Wistar rats
Keywords: متابولیت واکنش پذیر; Antioxidants; Hepatoprotective; Reactive metabolite; Therapeutic; Lipid peroxidation
Mechanism-based inactivation of cytochrome P450 2B6 by isoimperatorin
Keywords: متابولیت واکنش پذیر; CE; collision energy; DMSO; dimethyl sulfoxide; EPI; enhanced product ion; GSH; glutathione; IDA; information-dependent acquisition; IIMP; isoimperatorin; LC; liquid chromatography; LC-MS/MS; liquid chromatography coupled to tandem mass spectrometry; MR
Detection of cysteine- and lysine-based protein adductions by reactive metabolites of 2,5-dimethylfuran
Keywords: متابولیت واکنش پذیر; Furan-containing compounds; 2,5-Dimethylfuran; Reactive metabolite; Protein adductions; Bromine-tagged reagentsALT, alanine transaminase; BBA, 4-bromobenzylamine; BBM, 4-bromobenzylmercaptan; BSA, bovine serum albumin; CE, collision energy; CXP, cell exit
Role of cytochrome P450-mediated metabolism and identification of novel thiol-conjugated metabolites in mice with phenytoin-induced liver injury
Keywords: متابولیت واکنش پذیر; ABT; 1-aminobenzotriazole; ALT; alanine aminotransferase; BSO; l-buthionine-(S,R)-sulfoximine; Cys; cysteine; DPH; phenytoin; γ-GCS; γ-glutamilcysteine synthetase; 4â²-HPPH; 5-(4â²-hydroxyphenyl)-5-phenylhydantoin; MDZ; midazolam; NAC; N-acetylcystein
A proposed mechanism for the adverse effects of acebutolol: CES2 and CYP2C19-mediated metabolism and antinuclear antibody production
Keywords: متابولیت واکنش پذیر; AO; aldehyde oxidase; ANA; antinuclear antibody; AADAC; arylacetamide deacetylase; BNPP; bis(4-nitrophenyl)phosphate; CES; carboxylesterase; CYP; cytochrome P450; DTNB; 5,5â²-dithiobis(2-nitrobenzoic acid); EDTA; ethylenediamine-N,N,Nâ²Nâ²-tetraacetic
Adduct formation of electrochemically generated reactive intermediates with biomolecules
Keywords: متابولیت واکنش پذیر; Adduct formation; Benzoquinone; Cysteine tagging; Drug metabolism; Electrochemistry; Mass spectrometry; Protein adduct; Protein identification; Protein modification; Reactive metabolite
Use of a systems model of drug-induced liver injury (DILIsym®) to elucidate the mechanistic differences between acetaminophen and its less-toxic isomer, AMAP, in mice
Keywords: متابولیت واکنش پذیر; Drug induced liver injury (DILI); Mechanistic model; Pharmacokinetic/pharmacodynamic (PKPD) model; Hepatotoxicity; Acetaminophen; AMAP; Reactive metabolite; Mice; Simulation; Paracetamol;
Coupling ultra-high-pressure liquid chromatography with mass spectrometry for in-vitro drug-metabolism studies
Keywords: متابولیت واکنش پذیر; ADC; Analog-to-digital converter; ADMET; Absorption, distribution, metabolism, excretion and toxicity; APCI; Atmospheric pressure chemical ionization; CYP; Cytochrome P450; DDI; Drug-drug interaction; DMPK; Drug metabolism and pharmacokinetics; DT; Dwell
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Strategies to eliminate reactive metabolites
Keywords: متابولیت واکنش پذیر; 11β-Hydroxysteroid dehydrogenase; 11β-HSD; PF-915275; Reactive metabolite; Bioactivation; Glutathione adduct; Diabetes; Inhibitor;
Structural modifications of a 3-methoxy-2-aminopyridine compound to reduce potential for mutagenicity and time-dependent drug-drug interaction
Keywords: متابولیت واکنش پذیر; Bioactivation; AMES positive; TDI; Toxicity; Electron rich heteroaryls; Kinase inhibitor; Reactive metabolite; Mutagenicity; Time dependent drug-drug interaction;
Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation
Keywords: متابولیت واکنش پذیر; Benzothiazole; Benzoxazole; Amodiaquine; Benzoheterocyclic; Antiplasmodial; Reactive metabolite; Quinone imine
Glutathione S-transferase pi trapping method for generation and characterization of drug-protein adducts in human liver microsomes using liquid chromatography-tandem mass spectrometry
Keywords: متابولیت واکنش پذیر; Reactive metabolite; Protein adduct; LC-MS; Covalent binding; Human liver microsomes;
In vitro bioactivation of bazedoxifene and 2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol in human liver microsomes
Keywords: متابولیت واکنش پذیر; Bazedoxifene; Raloxifene; Reactive metabolite; LC-MS/MS; Cytochrome P450;
Protein target discovery of drug and its reactive intermediate metabolite by using proteomic strategy
Keywords: متابولیت واکنش پذیر; Drug target; Reactive metabolite; Proteomics; Mass spectrometry
Cytotoxicity evaluation of reactive metabolites using rat liver homogenate microsome-encapsulated alginate gel microbeads
Keywords: متابولیت واکنش پذیر; Cytotoxicity test; Rat liver homogenate microsome; Gel microbeads; Encapsulation; Reactive metabolite
Evidence of the formation of direct covalent adducts of primaquine, 2-tert-butylprimaquine (NP-96) and monohydroxy metabolite of NP-96 with glutathione and N-acetylcysteine
Keywords: متابولیت واکنش پذیر; Primaquine; NP-96; Glutathione; N-Acetylcysteine; Reactive metabolite; LC-MS;
Risk assessment and mitigation strategies for reactive metabolites in drug discovery and development
Keywords: متابولیت واکنش پذیر; Reactive metabolite; Adverse drug reaction; Hepatotoxicity
Metabolite identification by liquid chromatography-mass spectrometry
Keywords: متابولیت واکنش پذیر; Drug development; Drug discovery; Early stage drug discovery; Liquid chromatography-mass spectrometry (LC-MS); Mass spectrometer; Metabolism; Metabolite identification (Met ID); Pharmacologically active; Pharmacologically toxic; Reactive metabolite
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: Role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats
Keywords: متابولیت واکنش پذیر; Reactive metabolite; Electrophile; Glutathione; Microsomes; Cytosol; Glutathione transferase; Pharmacokinetics
Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists
Keywords: متابولیت واکنش پذیر; Salmonella; Reactive metabolite; P450; DNA; Covalent binding; Glutathione; Cyanide; Amine
Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle
Keywords: متابولیت واکنش پذیر; Glucokinase; Diabetes; Enzyme activation; Pyridone; Reactive metabolite
Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: Retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct
Keywords: متابولیت واکنش پذیر; P450; Reactive metabolite; Oxidation; Crystal structure; Glutathione; Orbitrap; Mass spectrometry
Phase I to II cross-induction of xenobiotic metabolizing enzymes: A feedforward control mechanism for potential hormetic responses
Keywords: متابولیت واکنش پذیر; Hormesis; Bioactivation; Feedforward; Feedback; Overcompensation; Reactive metabolite; Xenobiotics; Nrf2
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): Structure–activity relationships and strategies for the elimination of reactive metabolite formation
Keywords: متابولیت واکنش پذیر; PYK2; FAK; Kinase; Osteoporosis; Bioactivation; Reactive metabolite
Structure–activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation
Keywords: متابولیت واکنش پذیر; Reactive metabolite; Bioactivation; NR2B; NMDA; Metabolic stability
A quantitative high-throughput trapping assay as a measurement of potential for bioactivation
Keywords: متابولیت واکنش پذیر; [14C]potassium cyanide; Reactive metabolite; Covalent binding
Selection of new chemical entities with decreased potential for adverse drug reactions
Keywords: متابولیت واکنش پذیر; Bioactivation; Hepatotoxicity; Reactive metabolite