Tag: M.W=300-350

Takahashi, Kazunobu published the artcileDetermination of release rate of pyridine-triphenylborane (PTPB) from copper-free antifouling paints, COA of Formula: C23H20BN, the publication is Shikizai Kyokaishi (2005), 78(2), 50-57, database is CAplus.

Pyridine-triphenylborane (PTPB) is one of the alternative tin-free antifoulants in marine antifouling paints and was used widely in com. copper-free self-polishing antifouling paints in Japan. Anal. method for determination of PTPB at low ppb level in seawater was developed by HPLC with UV detection at 220 nm after pre-concentration with C18 solid-phase extraction (SPE). PTPB leached from an antifouling paint film was extracted from artificial seawater using a C18 solid-phase extraction (SPE) cartridge, and eluted with acetonitrile/pyridine (99:1). The recoveries of PTPB (25 μg/1 and 50 μg/l) spiked into artificial seawater were 96% and 97%, resp. The limit of determination of PTPB using 100 mL of artificial seawater was 0.5 μg/l for this anal. method. The HPLC-UV using SPE was applied onto measurement of the release rate (μg/cm²/day) of PTPB from copper-free antifouling paints containing PTPB according to both ISO 15181-1 and 15181-2.

Shikizai Kyokaishi published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C6H12N2O, COA of Formula: C23H20BN.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Kaburaki, Soyoko published the artcileHepatic drug metabolism in older people with body composition changes., Related Products of pyridine-derivatives, the publication is Geriatrics & gerontology international (2022), 22(5), 449-454, database is MEDLINE.

AIM: Dosage adjustment is essential in older individuals because they are prone to experience a decline in liver function and changes in body composition. However, quantitative tests or equations for evaluating the activity of hepatic drug metabolism have not yet been clearly established. We examined hepatic drug metabolism activities in older individuals, focusing on changes in body composition parameters. METHODS: Lansoprazole and nifedipine, substrates of the metabolic enzymes cytochrome P450 (CYP) 2C19 and 3A4, respectively, were selected to study hepatic drug metabolism. Residual samples from blood test for older patients were evaluated to determine drug metabolism. The body composition of relevant patients was determined by analyzing characteristic parameters of skeletal muscle mass index (SMI), handgrip strength (HGS) and hepatic steatosis index (HSI). The differences in hepatic drug metabolism were studied statistically among categories in terms of the cut-off value of these parameters. RESULTS: Older male patients receiving lansoprazole and nifedipine in the low SMI (<7.0 kg/m² ) category showed an 85-90% reduction in respective CYP2C19 and CYP3A4 metabolic activities compared with the normal SMI category. For the female patients, CYP2C19 and CYP3A4 metabolic activities showed no significant correlation with SMI and HGS. Fatty liver disease (HSI ≥36) was found to reduce CYP2C19 metabolic activity particularly in older female patients. CONCLUSIONS: Low CYP2C19 metabolic activity was statistically correlated with low SMI in male patients and high HSI in female patients, whereas low CYP3A4 metabolic activity was statistically correlated with low HGS in male patients. Geriatr Gerontol Int 2022; 22: 449-454.

Geriatrics & gerontology international published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Naito, Yasuyuki published the artcileConstructing vascularized hepatic tissue by cell-assembled viscous tissue sedimentation method and its application for vascular toxicity assessment, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Acta Biomaterialia (2022), 275-288, database is CAplus and MEDLINE.

In vitro Construction of the liver sinusoidal structure using artificial tissue is an important but worthwhile challenge, particularly for assessing the risk of diseases such as sinusoidal obstruction syndrome (SOS). Current models are unsuitable for evaluating the toxicity because of lacking sinusoidal capillary. In this study, we developed a vascularized hepatic tissue (VHT) using a unique tissue engineering technique, the cell assembled viscous tissue by sedimentation (CAViTs) method. The “viscous bodies” created using the CAViTs method exhibited significant self-assembly within 6 h after seeding, promoting cell-cell interaction. The level of albumin secreted by the VHT was four times higher than that of 2D-coculture and maintained for 1 mo. The gene expression pattern of the VHT was closer to that of total human liver, compared with the 2D system. Quant. evaluations of the vascular structure of VHT treated with two typical SOS-inducing compounds, monocrotaline and retrorsine, revealed higher sensitivity (IC50 = 40.35μM), 19.92 times higher than the cell-viability assay. Thus, VHT represents an innovative in vitro model that mimics the vessel network structure and could become a useful tool for the early screening of compounds associated with a risk of vascular toxicity. Mimicking sinusoidal structures in in vitro liver model is important to consider from the perspective of predicting hepatotoxicity such like sinusoidal obstruction syndrome (SOS). However, it was difficult to reconstruct the vascular structure within the hepatocyte-rich environment. In this study, we constructed a vascularized hepatic tissue in a high-throughput manner by a unique method using collagen and heparin, and evaluated its applicability to toxicity assessment. Vessel morphol. anal. of the model treated by monocrotaline, which is a well-known SOS-inducing compound, could predict the toxicity with higher sensitivity. To the best of our knowledge, this is the first report to provide vascularized hepatic tissues using sinusoidal endothelial cells at least for demonstrating applicability to the evaluation of SOS induction risk.

Acta Biomaterialia published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Hong, Bing published the artcileSedimentary spectrum and potential ecological risks of residual pharmaceuticals in relation to sediment-water partitioning and land uses in a watershed, Quality Control of 21829-25-4, the publication is Science of the Total Environment (2022), 152979, database is CAplus and MEDLINE.

Pharmaceutical residues in river surficial sediment are prone to anthropogenic impacts and environmental factors in watershed, but the mechanisms remain unclear. This study attempted to reveal surficial sediment-water pseudo-partitioning and anthropogenic (land use) patterns of pharmaceutical residues in surficial sediment among 23 subwatersheds of Jiulong River, southeast China with a gradient of urban land use percentile in dry and wet seasons. Thirty-eight out of target 86 compounds from six-category pharmaceuticals were quantified and ranged from below the quantification limits (0.001 mg kg^-1 dry mass) up to 8.19 mg kg^-1 dry mass (chlortetracycline) using a developed SPE-HPLC-MS/MS protocol. Antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs) collectively dominated sedimentary pharmaceutical residues for 34.5-99.8% of the total quantified compounds (median at 92%). Land uses in subwatersheds showed high consistency with sedimentary pharmaceutical residues in the dry season rather than the wet season, especially for human use only and veterinary use only compounds Surficial sediment-water partitioning of pharmaceutical compounds influenced their sedimentary residues regardless of season, which were determined by properties of compound and surficial sediment interactively. All tetracycline compounds, trimethoprim (sulfonamides synergist), caffeine (central nervous system drug), and oxfendazole (antiparasitic drug) were quantified to pose high potential ecol. risks to aquatics. Findings of this study suggest that pseudo-persistent legacy of human and veterinary pharmaceuticals requires a wider coverage of pharmaceutical compounds for a comprehensive ecol. assessment in the environment and more involvement of anthropogenic impacts and socioeconomic factors in the future studies.

Science of the Total Environment published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Quality Control of 21829-25-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Fukushi, Keiichi published the artcileSimultaneous determination of a pyridine-triphenylborane anti-fouling agent and its estimated degradation products using capillary zone electrophoresis, Application of Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Journal of Chromatography A (2010), 1217(14), 2187-2190, database is CAplus and MEDLINE.

A com. organoborane compound, pyridine-triphenylborane (PTPB), is often applied to ship hulls as an anti-fouling agent. The authors developed capillary zone electrophoresis (CZE) with direct UV detection for the simultaneous determination of PTPB and its estimated degradation products: diphenylborinic acid (DPB), phenylboronic acid (MPB), and phenol. The limits of detection (LODs) for PTPB, DPB, MPB, and phenol were, resp., 25, 30, 50, and 29 μg/L at a signal-to-noise ratio of three. At concentrations of 0.5 mg/L, values of the relative standard deviation (relative standard deviation, n = 6, intra-day) of peak area were obtained, resp., for PTPB, DPB, MPB, and phenol, as 4.1%, 4.1%, 4.7%, and 3.4% for peak heights 3.6%, 3.2%, 1.7%, and 1.4%, and for migration times 1.1%, 1.1%, 1.0%, and 0.73%. The analytes were detected within 14 min. Simple photodegradation experiments were conducted to verify the usefulness of the proposed method for addnl. PTPB degradation studies.

Journal of Chromatography A published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Application of Triphenyl(pyridin-1-ium-1-yl)borate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Kaewchuay, Netnapit published the artcileA novel hybrid mode of sample injection to enhance CZE sensitivity for simultaneous determination of a pyridine-triphenylborane anti-fouling agent and its degradation products, Synthetic Route of 971-66-4, the publication is Electrophoresis (2011), 32(12), 1486-1491, database is CAplus and MEDLINE.

We developed a novel hybrid sample injection mode (HSIM) that presents the combination of electrokinetic injection and vacuum injection to enhance detection sensitivity in CZE. Samples were introduced using both vacuum and electrokinetic injections simultaneously, with a water plug injected into the capillary prior to sample introduction (i.e. similarly to field-amplified sample injection, FASI). Using a sample mixture containing an anti-fouling agent applied to ship hulls, pyridine-triphenylborane and its degradation products (diphenylborinic acid, phenylboronic acid, and phenol) dissolved in ACN, the length of water plug, time, and voltage for sample introduction were optimized. The signal intensity (peak height) was found to be up to a 30-fold increased using HSIM by applying 4 kV for 4 s at the inlet end of the capillary as the cathode with supplementary vacuum in comparison with only vacuum injection for 4 s. The LODs (at a S/N of 3) for pyridine-triphenylborane, diphenylborinic acid, phenylboronic acid, and phenol were 0.88, 1.0, 21, and 23 μg/L, resp. At the level of 0.04 mg/L, the RSDs (n=4, intra-day) for the above analytes were in the ranges of 1.9-11, 4.3-9.2, and 0.34-0.66% for peak area, peak height, and migration time, resp. The HSIM is a simple and promising procedure useful for enhancing the sensitivity for both low-and high-mobility ions in CZE.

Electrophoresis published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Synthetic Route of 971-66-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Mikami, Eiichi published the artcileRapid determination of drugs in pharmaceutical preparations by liquid chromatography. (III). Determination of todralazine hydrochloride, trimetoquinol hydrochloride, nicardipine hydrochloride, sulpiride, furosemide and betahistine mesilate in pharmaceutical preparations, Formula: C10H20N2O6S2, the publication is Iyakuhin Kenkyu (1992), 23(6), 896-901, database is CAplus.

Liquid chromatog. methods using UV detection are described for determination of the title drugs in pharmaceutical preparations Stationary phase was Wakosil 5C18. Internal standards were p-hydroxybenzoic acid (for todralazine hydrochloride and sulpiride), Me p-aminobenzoate (for trimetoquinol hydrochloride and betahistidine mesilate), Pr p-hydroxybenzoate (for nicardipine hydrochloride), and Pr p-aminobenzoate (for furosemide). These rapid methods are useful for anal. for com. pharmaceutical preparations

Iyakuhin Kenkyu published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C10H20N2O6S2, Formula: C10H20N2O6S2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Motomura, Naoki published the artcileVisualization of calcium channel blockers in human adrenal tissues and their possible effects on steroidogenesis in the patients with primary aldosteronism (PA), Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Steroid Biochemistry and Molecular Biology (2022), 106062, database is CAplus and MEDLINE.

Voltage-gated L-type calcium channel (CaV) isoforms are well known to play pivotal tissue-specific roles not only in vasoconstriction but also in adrenocortical steroidogenesis including aldosterone biosynthesis. Alpha-1C subunit calcium channel (CC) (CaV1.2) is the specific target of anti-hypertensive CC blockers (CCBs) and its Alpha-1D subunit (CaV1.3) regulates depolarization of cell membrane in aldosterone-producing cells. Direct effects of CCBs on aldosterone biosynthesis were previously postulated but their intra-adrenal distribution and effects on steroid production in primary aldosteronism (PA) patients have remained virtually unknown. In this study, frozen tissue specimens constituting tumor, adjacent adrenal gland and peri-adrenal adipose tissues of nine aldosterone-producing adenoma (APA) cases were examined for visualization of amlodipine and aldosterone themselves using matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI). Liquid chromatog.-mass spectrometry (LC-MS) anal. was also performed to quantify amlodipine and 17 adrenal steroids in those cases above and compared the findings with immunohistochem. anal. of steroidogenic enzymes and calcium channels (CaV1.2 and CaV1.3). Effects of amlodipine on mRNA level of aldosterone biosynthetic enzymes were also explored using human adrenocortical carcinoma cell line (H295R). Amlodipine-specific peak (m/z 407.1 > 318.1) was detected only in amlodipine treated cases. Accumulation of amlodipine was marked in adrenal cortex compared to peri-adrenal adipose tissues but not significantly different between APA tumors and adjacent adrenal glands, which was subsequently confirmed by LC-MS quantification. Intra-adrenal distribution of amlodipine was generally consistent with that of CCs. In addition, quant. steroid profiles using LC-MS and in vitro study demonstrated the lower HSD3B activities in amlodipine treated cases. Immunoreactivity of CaV1.2 and HSD3B2 were also correlated. We report the first demonstration of specific visualization of amlodipine in human adrenal tissues by MALDI-MSI. Marked amlodipine accumulation in the adrenal glands suggested its direct effects on steroidogenesis in PA patients, possibly targeting on CaV1.2 and suppressing HSD3B activity.

Journal of Steroid Biochemistry and Molecular Biology published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Duan, Jingli published the artcileBioequivalence of domestic and imported betahistine mesylate tablets in healthy volunteers, Product Details of C10H20N2O6S2, the publication is Zhongguo Linchuang Yaolixue Zazhi (2003), 19(1), 42-45, database is CAplus.

The objective of this study was to determine the bioequivalence of domestic and imported betahistine mesylate in 20 healthy volunteers. A single dose of 24 mg domestic and imported betahistine mesylate tablets was given according to an open randomized 2-way crossover design. Plasma concentration of the main metabolite of betahistine, pyridine-2-ethanoic acid, was determined by HPLC/MS/MS method. The pharmacokinetics parameters of the two products were as follow: C_max 308.6 ± 208.8 mg L^-1 and 339.4 ± 213.4 mg L^-1; t_max 1.13 ± 0.66 h and 0.98 ± 0.47 h; AUC_0-t 1168.5 ± 794.9 mg L^-1 and 1129.3 ± 725.2 mg L^-1; AUC_0-∞ were 1213.2 ± 819.2 mg L^-1 and 1178.9 ± 752.5 mg L^-1, resp. The relative bioavailability of domestic product was (106.3 ± 29.1%). The results demonstrated that the two formations were bioequivalent by anal. of variance, two-one side test and 90% internal confidence.

Zhongguo Linchuang Yaolixue Zazhi published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C10H20N2O6S2, Product Details of C10H20N2O6S2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Jahed, Zeinab published the artcileNanocrown electrodes for parallel and robust intracellular recording of cardiomyocytes, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Nature Communications (2022), 13(1), 2253, database is CAplus and MEDLINE.

Drug-induced cardiotoxicity arises primarily when a compound alters the electrophysiol. properties of cardiomyocytes. Features of intracellular action potentials (iAPs) are powerful biomarkers that predict proarrhythmic risks. In the last decade, a number of vertical nanoelectrodes have been demonstrated to achieve parallel and minimally-invasive iAP recordings. However, the large variability in success rate and signal strength have hindered nanoelectrodes from being broadly adopted for proarrhythmia drug assessment. In this work, we develop vertically-aligned nanocrown electrodes that are mech. robust and achieve > 99% success rates in obtaining intracellular access through electroporation. We validate the accuracy of nanocrown electrode recordings by simultaneous patch clamp recording from the same cell. Finally, we demonstrate that nanocrown electrodes enable prolonged iAP recording for continual monitoring of the same cells upon the sequential addition of four incremental drug doses. Our technol. development provides an advancement towards establishing an iAP screening assay for preclin. evaluation of drug-induced arrhythmogenicity.

Nature Communications published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem