Category: 72509-76-3

Moreau, Magali published the artcileA baseline assessment of emerging organic contaminants in New Zealand groundwater, Product Details of C18H19Cl2NO4, the main research area is emerging organic contaminant baseline assessment groundwater pollution New Zealand; Emerging organic contaminant; Groundwater; Groundwater quality; Monitoring; New Zealand; Waikato region.

Emerging organic contaminants (EOC) are manufactured compounds, used for a variety of purposes, are a rising concern for freshwater quality and human and aquatic health. Their occurrence in groundwater was demonstrated in several international surveys. This work conducted the first baseline survey on EOC occurrence in New Zealand groundwater, using a wide-screening approach (723 compounds) and a novel stratified to mean residence time (MRT) randomized design to inform future monitoring. A total of 61 sites were sampled: 51 baseline sites from State of the Environment network in the Waikato region, and 10 targeted sites near known EOC sources for comparison. EOC were detected at 91% of baseline sites at concentrations of 0.1-11,000 ng/L. Multiple EOC groups were encountered: pesticides (48 compounds), pharmaceuticals (11), industrial (10), preservatives/food additives (3), and personal care products (1). Similar EOC diversity and concentration range were observed at targeted sites, with the addition of drugs of abuse and life-style compounds EOC detections occurred across young (1-11 yr. MRT), intermediate (11-50 yr. MRT), and old (50-250 yr. MRT) groundwater with higher concentrations and more types of EOC detected at sites with the youngest groundwater. Concentrations of 73 compounds detected at baseline sites were comparable to those observed in overseas groundwater, with 28 compounds measured at concentrations greater than the European Union maximum admissible concentration for pesticides. Survey results were used to: review current pesticide monitoring; propose complementary monitoring; identify potential EOC groundwater tracers; and identify compounds for which cost-effective, national laboratory capability is needed. Waikato survey results demonstrated ubiquitous occurrence of un-monitored, unregulated EOC in groundwater and limitations for using targeted approaches to establish monitoring.

Science of the Total Environment published new progress about Aquifers. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Product Details of C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Udumyan, Ruzan published the artcileBeta-blocker use and lung cancer mortality in a nationwide cohort study of patients with primary non-small cell lung cancer, Category: pyridine-derivatives, the main research area is non small cell lung cancer mortality beta blocker.

β-Adrenergic receptor blockers have been associated with improved survival among patients with different types of malignancies, but available data for patients with non-small cell lung cancer are contradictory and limited to small hospital-based studies. We aimed to investigate whether β-blocker use at time of cancer diagnosis is associated with lung cancer mortality in largest general population-based cohort of patients with NSCLC to date. For this retrospectively defined nationwide cohort study, we used prospectively collected data from Swedish population and health registers. Through Swedish Cancer Register, we identified 18,429 patients diagnosed with primary NSCLC between 2006 and 2014 with follow-up to 2015. Cox regression was used to estimate the association between β-blocker use at time of cancer diagnosis ascertained from the Prescribed Drug Register and cancer-specific mortality identified from the Cause of Death Register. Over a median follow-up of 10.2 mo, 14,994 patients died. Compared with nonuse, β-blocker use was not associated with lung cancer mortality [HR (95% confidence interval): 1.01 (0.97-1.06)]. However, the possibility that diverging associations for specific β-blockers and some histopathol. subtypes exist cannot be excluded. In this nationwide cohort of patients with NSCLC, β-blocker use was not associated with lung cancer mortality when assessed in aggregate in the total cohort, but evidence for some β-blockers is less conclusive.

Cancer Epidemiology, Biomarkers & Prevention published new progress about Diagnosis. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fagerberg, Jonas Henrik published the artcileAffinity of Lipophilic Drugs to Mixed Lipid Aggregates in Simulated Gastrointestinal Fluids, Computed Properties of 72509-76-3, the main research area is sodium taurocholate affinity lipophilic lipid aggregate simulated gastrointestinal fluid; Affinity; Biorelevant dissolution media; Drug lipophilicity; Ionization; Mixed lipid aggregates; Solubilization.

Mixed lipid aggregates, comprising of bile salts and phospholipids, present in the small intestine assist in drug solubilization and subsequent drug dissolution and absorption through the intestinal epithelium. The increased variability in their levels, observed physiol., may create challenges not only for in vivo bioavailability and bioequivalence studies, but also for in vitro bio-predictive studies as correlations between in vitro and in vivo data are not always successful. The current study investigated the impact of biorelevant dissolution media, with physiol. relevant sodium taurocholate and lecithin levels, on the apparent solubility and affinity of lipophilic compounds with a wide range of physicochem. properties (drug ionization, drug lipophilicity, mol. weight) to mixed lipid aggregates. Apparent solubility data in biorelevant dissolution media for the studied neutral drugs, weak bases and weak acids were compared against a phosphate buffer pH 6.5 in the absence of these lipidic components. Presence of mixed lipid aggregates enhanced the apparent solubility of the majority of compounds and the use of multivariate data anal. identified the significant parameters affecting drug affinity to mixed lipid aggregates based on the chem. class of the drug. For neutral drugs, increasing bile salt concentrations and/or drug lipophilicity resulted in greater enhancement in apparent solubility at 24-h. For weak bases and weak acids, the effect of increasing bile salt levels on apparent solubility depended mostly on an interplay between drug lipophilicity and drug ionization.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Affinity. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lin, Yi-Sian published the artcileGWAS Meta-Analysis Reveals Shared Genes and Biological Pathways between Major Depressive Disorder and Insomnia, SDS of cas: 72509-76-3, the main research area is major depressive disorder insomnia gene biol pathway metaanalysis; GWAS; MDD; STRING; comorbidity; eQTL; gene network; insomnia; meta-analysis.

Major depressive disorder (MDD) is one of the most prevalent and disabling mental disorders worldwide. Among the symptoms of MDD, sleep disturbance such as insomnia is prominent, and the first reason patients may seek professional help. However, the underlying pathophysiol. of this comorbidity is still elusive. Recently, genome-wide association studies (GWAS) have begun to unveil the genetic background of several psychiatric disorders, including MDD and insomnia. Identifying the shared genomic risk loci between comorbid psychiatric disorders could be a valuable strategy to understanding their comorbidity. This study seeks to identify the shared genes and biol. pathways between MDD and insomnia based on their shared genetic variants. First, we performed a meta-anal. based on the GWAS summary statistics of MDD and insomnia obtained from Psychiatric Genomics Consortium and UK Biobank, resp. Next, we associated shared genetic variants to genes using two gene mapping strategies: (a) positional mapping based on genomic proximity and (b) expression quant. trait loci (eQTL) mapping based on gene expression linkage across multiple tissues. As a result, a total of 719 shared genes were identified. Over half (51%) of them are protein-coding genes. Functional enrichment anal. shows that the most enriched biol. pathways are related to epigenetic modification, sensory perception, and immunol. signatures. We also identified druggable targets using a network approach. Together, these results may provide insights into understanding the genetic predisposition and underlying biol. pathways of comorbid MDD and insomnia symptoms.

Genes published new progress about Cerebellum. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, SDS of cas: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Brinkmann, Joscha published the artcileIn-Silico Screening of Lipid-Based Drug Delivery Systems, Application In Synthesis of 72509-76-3, the main research area is lipid based drug delivery system screening formulation; PC-SAFT; lipid-based formulations; solubility; thermodynamic modeling.

This work proposes an in-silico screening method for identifying promising formulation candidates in complex lipid-based drug delivery systems (LBDDS). The approach is based on a min. amount of exptl. data for API solubilites in single excipients. Intermol. interactions between APIs and excipients as well as between different excipients were accounted for by the Perturbed-Chain Statistical Associating Fluid Theory. The approach was applied to the in-silico screening of lipid-based formulations for ten model APIs (fenofibrate, ibuprofen, praziquantel, carbamazepine, cinnarizine, felodipine, naproxen, indomethacin, griseofulvin and glibenclamide) in mixtures of up to three out of nine excipients (tricaprylin, Capmul MCM, caprylic acid, Capryol 90, Lauroglycol FCC, Kolliphor TPGS, polyethylene glycol, carbitol and ethanol). For eight out of the ten investigated model APIs, the solubilities in the final formulations could be enhanced by up to 100 times compared to the solubility in pure tricaprylin. Fenofibrate, ibuprofen, praziquantel, carbamazepine are recommended as type I formulations, whereas cinnarizine and felodipine showed a distinctive solubility gain in type II formulations. Increased solubility was found for naproxen and indomethacin in type IIIb and type IV formulations. The solubility of griseofulvin and glibenclamide could be slightly enhanced in type IIIb formulations. The exptl. validation agreed very well with the screening results. The API solubility individually depends on the choice of excipients. The proposed in-silico-screening approach allows formulators to quickly determine most-appropriate types of lipid-based formulations for a given API with low exptl. effort.

Pharmaceutical Research published new progress about Cosolvents. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dantonio, Alyssa L. published the artcileIntersystem extrapolation factors are substrate-dependent for CYP3A4: impact on cytochrome P450 reaction phenotyping, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is intersystem extrapolation factor CYP3A4 reaction phenotyping pharmacokinetics.

The use of intersystem extrapolation factors (ISEF) is required for the quant. scaling of drug metabolism data generated in individually expressed cytochrome P 450 (CYP) enzymes when estimating fractional contribution (fm) to metabolism by P 450 enzymes in vivo. For successful prediction of fm, ISEF values must be universal across all substrates for any individual enzyme. In this study, ISEF values were generated for ten CYP3A4 selective substrates using a common source of recombinant heterologously expressed CYP3A4 (rCYP) and a pool of human liver microsomes. The resulting ISEF values for CYP3A4 were substrate-dependent and ranged 8-fold, with the highest value generated from intrinsic clearance of midazolam depletion (0.36) and the lowest from quinidine depletion (0.044). Application of these ISEF values for estimation of the fractional contribution of CYP3A4 and CYP2C19 to omeprazole clearance yielded values that ranged from 0.21-0.63 and 0.37-0.79, resp., as compared with back-extrapolated in vivo fm values of 0.27 (CYP3A4) and 0.85 (CYP2C19) from clin. pharmacokinetic data. For risperidone, estimated fm values for CYP3A4 and CYP2D6 ranged from 0.87-0.98 and 0.02-0.13, resp., as compared with in vivo values of 0.36 (CYP3A4) and 0.63-0.88 (CYP2D6), showing that the importance of CYP3A4 was overestimated, and the importance of CYP2D6 underestimated. Overall, these findings suggest that ISEF values for CYP3A4 can vary with the marker substrate used to derive them, thereby reducing the effectiveness of the approach of using metabolism data from rCYP3A4 with ISEF values for the prediction of fraction metabolized values in vivo.

Drug Metabolism & Disposition published new progress about Hepatocyte. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Feifei published the artcileAssociation between potentially inappropriate medication and adverse drug reactions in hospitalized elderly patients, HPLC of Formula: 72509-76-3, the main research area is potentially inappropriate medication adverse drug reaction hospitalized human; adverse drug reactions; hospitalized; inappropriate medicine.

The Beers, European Union (EU) and Screening Tool of Older Persons’ potentially inappropriate Prescription (STOPP) criteria were developed to improve the safe use of medicines in the elderly. However, the predictive validity of existing criteria to detect adverse drug reactions (ADRs) remains unexplored. The objective of the current study was to determine whether the 2019 Beers, 2015 STOPP or 2015 EU potentially inappropriate medicine (PIM) criteria were associated with ADRs. A retrospective, cross-sectional investigation was conducted among older persons (â‰?0 years of age) admitted to a tertiary hospital in China between Apr. 2019 and Dec. 2019. PIMs were identified as per the Beers, EU and STOPP criteria definitions. ADRs were retrospectively evaluated by two clin. pharmacists using the Naranjo algorithm. Multivariate logistic regression was used to evaluate the factors associated with ADRs in the hospitalized patients. The study participants included 560 hospitalized patients (mean age 72.05 8.15). The prevalence of patients receiving at least one PIM was 52.1%, 37.0% and 42.9% according to the Beers, EU and STOPP criteria, resp. Univariate anal. showed that ADRs were associated with PIMs listed in the Beers criteria (OR: 2.093, 95% CI: 1.028-4.263, 0.042), but not with the STOPP-listed (OR: 0.536, 95% CI: 0.255-1.123, 0.098) and EU-listed PIMs (OR: 0.258, 95% CI: 0.118-0.563, 0.001). In contrast to the STOPP and EU criteria on PIMs, the Beers criteria were significantly associated with avoidable ADRs in hospitalized older persons.

Journal of Clinical Pharmacy and Therapeutics published new progress about Algorithm. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, HPLC of Formula: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yu, Yong-Jie published the artcileAutomatic data analysis workflow for ultra-high performance liquid chromatography-high resolution mass spectrometry-based metabolomics, COA of Formula: C18H19Cl2NO4, the main research area is automatic data analysis algorithm UHPLC HRMS metabolomics; Automatic data analysis; Chemometrics; MATLAB GUI; UPLC-HRMS; Untargeted metabolomics.

Data anal. for ultra-performance liquid chromatog. high-resolution mass spectrometry-based metabolomics is a challenging task. The present work provides an automatic data anal. workflow (AntDAS2) by developing three novel algorithms, as follows: (i) a d.-based ion clustering algorithm is designed for extracted-ion chromatogram extraction from high-resolution mass spectrometry; (ii) a new maximal value-based peak detection method is proposed with the aid of automatic baseline correction and instrumental noise estimation; and (iii) the strategy that clusters high-resolution m/z peaks to simultaneously align multiple components by a modified dynamic programing is designed to efficiently correct time-shift problem across samples. Standard compounds and complex datasets are used to study the performance of AntDAS2. AntDAS2 is better than several state-of-the-art methods, namely, XCMS Online, Mzmine2, and MS-DIAL, to identify underlying components and improve pattern recognition capability. Meanwhile, AntDAS2 is more efficient than XCMS Online and Mzmine2. A MATLAB GUI of AntDAS2 is designed for convenient anal. and is available at the following webpage: http://software.tobaccodb.org/software/antdas2.

Journal of Chromatography A published new progress about Algorithm. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lu, Yang published the artcileEnhanced felodipine dissolution from high drug loading amorphous solid dispersions with PVP/VA and sodium dodecyl sulfate, Application In Synthesis of 72509-76-3, the main research area is felodipine dissolution amorphous solid dispersion sodium dodecyl sulfate PVP.

The objective of this study was to investigate the mechanisms of sodium dodecyl sulfate (SDS) and Copovidone (PVP/VA) enhancing the dissolution of high loaded felodipine (FLDP) amorphous extrudates. The rheol. results indicated that PVP/VA inhibited FLDP crystallization and the binary FLDP-PVP/VA (1:1 and 1:3) and ternary FLDP-PVP/VA-SDS (1:1:0.02-0.16 and 1:3:0.02-0.32) extrudates were amorphous solid dispersions (ASDs). Internal SDS (5%-20%) decreased glass transition temperature (Tgs) of FLDP-PVP/VA ternary ASDs. The enhanced dissolution rate of binary or ternary PVP/VA-rich ASDs in the non-sink condition of 0.05%SDS was achieved. SDS enhanced the dissolution of PVP/VA-rich ASDs via wettability and complexation with PVP/VA to accelerate the medium uptake and erosion kinetics of extrudates, but induced FLDP recrystallization and resulted in incomplete dissolution of FLDP-rich extrudates. Interestingly, when the ratio of FLDP-SDS was 1:0.08-0.12, the addition of SDS can significantly promote drug dissolution To confirm the in vitro relevance of these mol. interaction mechanisms, we prepared two tablet formulations which internal or external added SDS, resp., the ratio of FLDP-SDS was 1:0.1. The results show that SDS can promote the dissolution of FLDP when only SDS was internal added.

Journal of Drug Delivery Science and Technology published new progress about Absorption. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Premkumar, B. published the artcileFormulation and evaluation of Felodipine hollow microspheres, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is blood pressure heart stroke felodipine hollow microsphere biocompatibility stability.

Felodipine is a calcium channel blocker which is used for the treatment of high blood pressure to prevent heart stroke. In the current research work hollow microspheres of Felodipine with better absorption in gastric pH was formulated by using various polymers. Drug polymer compatibility was characterized by FT-IR. Microspheres were prepared by emulsion solvent diffusion technique by using different polymers such as Et cellulose, carbopol 934, eudragit and sodium alginate at varying concentrations The formulations were evaluated for micromeritic properties, buoyancy, percentage yield, entrapment efficiency, in vitro studies and stability stuides. SEM photographs showed outer surface of microspheres was smooth and dense where as internal surface was porous which helped to prolong floating. Optimized F2 formulation exhibited higher release rate 95.55%. In vitro drug release studies showed controlled release of Felodipine for over 8h. Stability studies indicated the F2 formulation was stable with respect to its drug release.

European Journal of Biomedical and Pharmaceutical Sciences published new progress about Absorption. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem