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(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - November 17, 2017 Category: Drugs & Pharmacology Source Type: research
Acknowledgements to reviewers
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
The Metabolism of Methazolamide in Immortalized Human Keratinocytes, HaCaT Cells
Conclusion: N-[3-methyl-5-sulfo-1,3,4-thiadiazol-2(3H)-ylidene]acetamide (MSO) is not considered to be a direct product of an enzymatic reaction, but rather an auto-oxidation product of N-[3-methyl-5- sulfe-1,3,4-thiadiazol-2(3H)-ylidene]acetamide, a chemically unstable sulfenic acid, which is produced by cytochrome P450 from the -lyase product of cysteine conjugate of methazolamide. MSO is considered to be susceptible to glutathione and to return to glutathione conjugate of methazolamide, forming a futile cycle. A hypothetical scenario is presented as to the onset of the disease. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Quantification of Etodolac in Human Plasma for Pharmacokinetics and Bioequivalence Studies in 27 Korean Subjects
Conclusion: Thus, the new testified method was successfully applied for the pharmacokinetic and bioequivalence studies for two etodolac formulations. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Variability of Zaleplon 5-Oxidase Activity in Mice and Humans, and Inhibition by Raloxifene
Conclusion: High inter-individual variability of ZAL 5-oxidase activity and potential for interaction of ZAL with other medicines that are inhibitors of aldehyde oxidase should be taken into consideration in clinical usage of ZAL. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Ortho-Methylarylamines as Time-Dependent Inhibitors of Cytochrome P450 1A1 Enzyme
Conclusion: Four compounds have been identified that exhibit selective time-dependent inhibition of P450 1A1. Modeling studies have indicated that the proximity of the aromatic methyl group to the heme-Fe could be the main contributor for time-dependent inhibition. Future studies will focus on the confirmation of the involvement of the aromatic methyl group in enzyme inactivation. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
A Novel Liquid Chromatography Tandem Mass Spectrometry Method for the Estimation of Bilirubin Glucuronides and its Application to In Vitro Enzyme Assays
Conclusion: We have developed a sensitive LC-MS/MS based method for the quantitation of bilirubin and its glucuronides from in vitro incubations. This method was successfully utilized to determine bilirubin glucuronidation kinetics in HLM and human rUGT1A1. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Genipin Inhibits the Induction of Inducible Nitric Oxide Synthase Through the Inhibition of NF-κB Activation in Rat Hepatocytes
Conclusion: Genipin influenced the induction of inflammatory mediators, iNOS and TNF-α, in part through the inhibition of NF-κB activation in hepatocytes. Genipin may have therapeutic potential for organ injuries including liver. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Strong Induction of Cytochrome P450 1A/3A, But not P450 2B, in Cultured Hepatocytes from Common Marmosets and Cynomolgus Monkeys by Typical Human P450 Inducing Agents
Conclusion: These results indicate that P450 1A/3A induction by typical human P450 inducers in hepatocytes from marmosets and/or cynomolgus monkeys are similar to those of humans (except for P450 2B induction by phenobarbital in humans), suggesting that marmosets and cynomolgus monkeys might be suitable models for evaluating the drug interactions in preclinical studies. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Cytochrome P450 2A6 Phenotyping Using Dietary Caffeine Salivary Metabolite Ratios and Genotyping Using Blood on Storage Cards in Non-smoking Japanese Volunteers
Background: A simple method of genotyping and phenotyping cytochrome P450 2A6 (CYP2A6) was previously reported using individual blood samples and urinary caffeine metabolite ratios of 1,7-dimethyluric acid (17U) to 1-methylxanthine (1X). Objective: Blood spotted onto storage cards and salivary caffeine metabolites were analyzed in 27 healthy non-smoking Japanese volunteers with no prior abstention from dietary caffeine intake. Methods: 1,7-Dimethylxanthine (17X), 17U, 1X, and caffeine levels in spot saliva samples were determined in Japanese non-smokers by high-performance liquid chromatography under normal dietary caffein...
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Pharmacokinetics, Metabolism and Disposition of [14C]XQ-1H After Intravenous Administration to Male Rats
Conclusion: Binding of XQ to RBCs may lower the blood’s viscosity and thus provide symptomatic improvement of ischemic stroke patients. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Meet Our Editorial Board Member
(Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - March 15, 2017 Category: Drugs & Pharmacology Source Type: research
Effect of Cardiovascular Injury on Catabolism of Adenosine and Adenosine 5-‘Triphosphate in Systemic Blood in a Freely Moving Rat Model In Vivo
Background: Previous studies have shown that catabolism of adenosine 5’-triphosphate (ATP) in red blood cell (RBC) may be a key factor for cardiovascular protection and maintaining cardiovascular homeostasis. Objective: To investigate the effect of cardiovascular injury on adenosine and ATP catabolism in systemic blood using a freely moving rat model in vivo. Method: After acclimatized to the experimental environment, Sprague Dawley (SD) rats were each given either isoproterenol (30 mg/kg) or saline (1 mL/kg) by subcutaneous (sc) injection. Blood samples were collected sequentially for up to 6 hours for measurement of re...
Source: Drug Metabolism Letters - October 1, 2016 Category: Drugs & Pharmacology Source Type: research
CYP2B6 and OPRM1 Receptor Polymorphisms at Methadone Clinics And Novel OPRM1 Haplotypes: A Cross-Sectional Study
Conclusion: C64T and G15631T in CYP2B6and G31A, G691C, and A118G in OPRM1were found to be polymorphic. The new haplotypes may give a new insight on methadone clinics. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - October 1, 2016 Category: Drugs & Pharmacology Source Type: research
UHPLC Quantitation Method for New Thiazolidinedione LPSF/GQ-02 and In Vitro/In Vivo Kinetic Studies
Conclusion: The intravenous pharmacokinetic parameters are in agreement with a good future posology, even though the plasma concentrations from oral administration were not quantifiable in a dose of 12 mg/kg. The preliminary safety study demonstrated no acute effect of the drug in liver and kidneys. The LPSF/GQ-02 is a new thiazolidinedione that should continue being evaluated for future clinical use. (Source: Drug Metabolism Letters)
Source: Drug Metabolism Letters - October 1, 2016 Category: Drugs & Pharmacology Source Type: research
