Category: 72509-76-3

Suriyapakorn, Bovornpat published the artcileComparison of potential drug-drug interactions with metabolic syndrome medications detected by two databases, Category: pyridine-derivatives, the main research area is atenolol bisoprolol enalapril imidapril antiplatelet antilipemic antihypertensive metabolic syndrome.

Drug-drug interactions (DDIs) are one of the most common drug-related problems. Recently, electronic databases have drug interaction tools to search for potential DDIs, for example, Micromedex and Drugs.com. However, Micromedex and Drugs.com have different abilities in detecting potential DDIs, and this might cause misinformation to occur between patients and health care providers. The aim of this study was to compare the ability of Micromedex and Drugs.com to detect potential DDIs with metabolic syndrome medications using the drug list from the U-central database, King Chulalongkorn Memorial Hospital in Apr. 2019. There were 90 available drugs for the treatment of the metabolic syndrome and its associated complications, but six were not found in the Micromedex and Drugs.com databases; therefore, only 84 items were used in the present study. There were 1,285 potential DDI pairs found by the two databases. Micromedex reported DDIs of 724 pairs, while, Drugs.com reported 1,122 pairs. For the severity of the potential DDI reports, the same severity occurred between the two databases of 481 pairs (37.43%) and a different severity for 804 pairs (62.57%). Drugs.com had a higher sensitivity to detect potential DDIs by approx. 1.5-fold, but Micromedex supplied more informative documentation for the severity classification. Therefore, pharmacists should use at least two databases to evaluate potential DDIs and determine the appropriate drug regimens for physician communications and patient consultations.

PLoS One published new progress about Antidiabetic agents. 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

Joyce, Paul published the artcileTIRF Microscopy-Based Monitoring of Drug Permeation Across a Lipid Membrane Supported on Mesoporous Silica, SDS of cas: 72509-76-3, the main research area is felodipine drug permeation lipid membrane mesoporous silica; drug delivery; membrane permeation; mesoporous silica; supported lipid bilayer; total internal reflection fluorescence.

There is an urgent demand for analytic approaches that enable precise and representative quantification of the transport of biol. active compounds across cellular membranes. In this study, we established a new means to monitor membrane permeation kinetics, using total internal reflection fluorescence microscopy confined to a �00 nm thick mesoporous silica substrate, positioned underneath a planar supported cell membrane mimic. This way, we demonstrate spatiotemporally resolved membrane permeation kinetics of a small-mol. model drug, felodipine, while simultaneously controlling the integrity of, and monitoring the drug binding to, the cell membrane mimic. By contrasting the permeation behavior of pure felodipine with felodipine coupled to the permeability enhancer caprylate (C8), we provide evidence for C8-facilitated transport across lipid membranes, thus validating the potential for this approach to successfully quantify carrier system-induced changes to cellular membrane permeation.

Angewandte Chemie, International Edition published new progress about Blood-brain barrier. 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

Zhang, Shujuan published the artcileBile acid transporter mediated STC/Soluplus self-assembled hybrid nanoparticles for enhancing the oral drug bioavailability, Synthetic Route of 72509-76-3, the main research area is sodium taurocholate Soluplus nanoparticle bioavailability bile acid transporter; ASBT; Felodipine; P4; Self-assembled hybrid nanoparticles; Sodium taurocholate; Soluplus.

The nano-particulate system for oral delivery faces a big challenge across the gastrointestinal bio-barriers. The aim was to explore the potential applications of bile acid transporter mediated the self-assembled hybrid nanoparticles (SHNPs) of sodium taurocholate (STC) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (Soluplus) for augmenting the oral delivery of poorly water-soluble drugs. Felodipine (FLDP) was chosen as a model drug. The self-assembly of STC with Soluplus to load FLDP and the microstructure of the SHNPs were confirmed using mol. simulation, STC determination by high performance liquid chromatog. (HPLC) and transmission electron microscope. Results showed that STC was integrated with Soluplus on the surface of nanoparticles by hydrophobic interactions. The permeability of FLDP loaded STC/Soluplus SHNPs was STC dependent in the ileum, which was inhibited by the higher concentrations of STC and the inhibitor of apical sodium-dependent bile acid transporter (ASBT). STC/Soluplus (1:9) SHNPs significantly improved the drug loading of FLDP, achieved the highest permeability of FLDP and realized 1.6-fold of the area under the curve (AUC) of Soluplus self-assembled nanoparticles (SNPs). A water-quenching fluorescent probe P4 was loaded into the STC/Soluplus SHNPs, which verified that the SHNPs were transferred intactly across the ileum. In conclusion, STC/Soluplus SHNPs via ASBT are a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Drug bioavailability. 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, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

El Sayed, Mira published the artcileInsights into Dissolution and Solution Chemistry of Multidrug Formulations of Antihypertensive Drugs, COA of Formula: C18H19Cl2NO4, the main research area is antihypertensive dissolution solubility supersaturation formulation; amorphous; fixed dose combinations; multidrug formulations; solubility; supersaturation.

Using fixed dose combinations of drugs instead of administering drugs sep. can be beneficial for both patients and the health care system, but the current understanding of how multidrug formulations work at the mol. level is still in its infancy. Here, we explore dissolution, solubility, and supersaturation of various drug combinations in amorphous formulations. The effect of chem. structural similarity on combination behavior was investigated by using structurally related compounds of both drugs. The effect of polymer type on solution behavior was also evaluated using chem. diverse polymers. Indapamide (IPM) concentration decreased when combined with felodipine (FDN) or its analogs, which occurred even when the IPM solution was undersaturated The extent of solubility decrease of FDN was less than that of IPM from the dissolution of an equimolar formulation of the drugs. No significant solubility decrease was observed for FDN at low contents of IPM which was also observed for other dihydropyridines, whereas FDN decreases at high contents of IPM. This was explained by the complex nature of the colloidal precipitates of the combinations which impacts the chem. potential of the drugs in solution at different levels. The maximum achievable concentration of FDN and IPM during dissolution of the polyvinylpyrrolidone-based amorphous solid dispersion was higher than the value measured with the hydroxypropyl methylcellulose acetate succinate-based formulation. This emphasizes the significance of mol. properties and chem. diversity of drugs and polymers on solution chem. and solubility profiles. These findings may apply to drugs administered as a single dosage form or in sep. dosage forms and hence need to be well controlled to assure effective treatments and patient safety.

Molecular Pharmaceutics published new progress about Amorphous materials. 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

Choudhari, Alap A. published the artcileMicroencapsulation of solid dispersions of felodipine and characterization of release mechanism, HPLC of Formula: 72509-76-3, the main research area is felodipine microencapsulation sustained release solid dispersion.

The study was aimed at increase the solubility of poorly soluble drug Felodipine and formulating it in sustained release dosage form. Solid dispersion of drug was prepared using Poly vinyl pyrollidone (PVP) and hydroxyl Pr Me cellulose (HPMC) as inert hydrophilic carriers by kneading method. A 17-fold increase in dissolution rate of Felodipine was observed with solid dispersion prepared with HPMC. Optimized solid dispersion was further characterized by Powder X-ray diffraction (PXRD) which suggest transformation of crystalline Felodipine in amorphous form and Fourier transform IR spectroscopy (FTIR) suggesting no possible interaction. Sustained release microcapsules of Felodipine were formulated using Et cellulose (EC) and Eudragit RL 100 (EDRL) as coating material with solid dispersion of Felodipine as core by emulsion solvent evaporation method. Gelatin was used as microencapsulating agent employing coacervation-phase separation technique. Microcapsules from all the batches were found to discrete, spherical and free flowing and % entrapment efficiency was found to be in range of 88% to 96%. All the batches of microcapsules showed sustained release curve in pH 7.4 phosphate buffer up to eight hours with microcapsules prepared with gelatin giving Felodipine release up to 86% after 8 h. XRD pattern studies of the microcapsules made of gelatin showed drug still present in the amorphous form and thus maintaining its solubility in the microcapsule system.

International Journal of Drug Development & Research published new progress about Amorphous materials. 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

Jiang, Ling published the artcileApplication of Enzymatic Promiscuity in Pharmaceutical Synthesis: Papain-catalyzed One-pot Synthesis of 1,4-Dihydropyridine Calcium Channel Antagonists and Derivatives, Computed Properties of 72509-76-3, the main research area is aryl aldehyde acetoacetate aminocrotonate papain catalyst three component reaction; phenyl dihydropyridine dicarboxylate preparation green chem.

A new method for the synthesis of 1,4-dihydropyridine(1,4-DHP) calcium channel antagonists felodipine, nitrendipine and their derivatives via papain-catalyzed three-component reactions of aldehyde, Me acetoacetate and Et 3-aminocrotonate was developed. Operational simplicity, mild reaction conditions and eco-friendliness are the key features of this protocol.

Chemical Research in Chinese Universities published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Wang, Zhengyong published the artcileUltrasonic extraction and nebulization in real-time coupled with carbon fiber ionization mass spectrometry for rapid screening of the synthetic drugs adulterated into herbal products, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is ultrasonic extraction nebulization direct analysis carbon fiber ionization; screening drug adulterated herbal product; Carbon fiber ionization; Direct analysis; Herbal products; Rapid screening; Synthetic drugs; Ultrasonic extraction and nebulization in real-time.

Ultrasonic extraction and nebulization in real-time/carbon fiber ionization mass spectrometry (UEN/CFI-MS) was developed to screen the synthetic drugs adulterated into herbal products such as antidiabetic drug, antihypertensive drug, and hypolipidemic drug. Recently, ambient ionization MS techniques have achieved great advance for rapid anal. of sample surface. However, direct anal. of the analytes inside samples remains a challenge due to a lack of effective online sample extraction procedures. Owing to disappointing desorption efficiency, analytes inside the sample suffer from low detecting sensitivity when applying ambient ionization MS techniques. In this study, online ultrasonic extraction combined with carbon fiber ionization was used for real-time extraction, nebulization and detection of the analytes inside samples. The ultrasonic atomizer could produce a high-frequency vibration to realize online extraction and nebulization of sample. Then, the produced sample droplets could be immediately ionized by the carbon fiber ionization mass spectrometry. UEN/CFI-MS has shown great compatibility to solvents and compounds with a wide range of polarity and has few limitations for the shape of sample. UEN/CFI-MS was successfully applied for the rapid screening of synthetic drugs adulterated into herbal products. Among 37 batches of herbal products, 1 batch of Chinese patent medicine and 6 batches of dietary supplements were detected to be adulterated with the synthetic chems. without labeling.

Analytica Chimica Acta published new progress about Carbon fibers Role: NUU (Other Use, Unclassified), USES (Uses). 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

Jiang, Ling published the artcileMechanochemical enzymatic synthesis of 1,4-dihydropyridine calcium antagonists and derivatives, Application In Synthesis of 72509-76-3, the main research area is Lipozyme ball milling dihydropyridine calcium antagonists.

BACKGROUND : Enzyme promiscuity has attracted significant attention from chemists and biochemists in recent years. However, long reaction time and use of toxic organic solvents limit its applications for industrial processes. 1,4-Dihydropyridine (1,4-DHP) calcium antagonists are recommended for the first line treatment of hypertension. Although some chem. protocols for the preparation of 1,4-DHP calcium antagonists have been developed, enzymic synthesis of these compounds still remains uncovered. RESULTS : Solvent-free quick synthesis of 1,4-DHP calcium antagonists felodipine, nitrendipine, nifedipine and nemadipine B and their derivatives was achieved by Lipozyme RM IM (triacylglycerol acylhydrolase, EC3.1.1.3)-catalyzed multicomponent reactions of aromatic aldehyde, alkyl acetoacetate and alkyl 3-aminocrotonate under ball-milling conditions. The products were obtained in moderate yields (up to 86.8%) and the influence of reaction conditions including catalyst loading, grinding auxiliary and grinding frequency was investigated. CONCLUSION : The protocol successfully overcame some longstanding problems in the field of enzymic promiscuity research, such as long reaction time and use of harmful organic solvents, and demonstrated the potential application value of promiscuous enzyme-catalyzed reactions under ball-milling conditions for pharmaceutical synthesis. © 2019 Society of Chem. Industry.

Journal of Chemical Technology and Biotechnology published new progress about Pharmaceutical natural products (1,4-Dihydropyridine calcium). 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

Ormerod, Kiel G. published the artcileRegulation of excitation-contraction coupling at the Drosophila neuromuscular junction, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Drosophila neuromuscular junction excitation contraction coupling; drosophila; neuromuscular junction; synapse.

The Drosophila neuromuscular system is widely used to characterize synaptic development and function. However, little is known about how specific synaptic alterations effect neuromuscular transduction and muscle contractility, which ultimately dictate behavioral output. Here we develop and use a force transducer system to characterize excitation-contraction coupling at Drosophila larval neuromuscular junctions (NMJs), examining how specific neuronal and muscle manipulations disrupt muscle contractility. Muscle contraction force increased with motoneuron stimulation frequency and duration, showing considerable plasticity between 5 and 40 Hz and saturating above 50 Hz. Endogenous recordings of fictive contractions revealed average motoneuron burst frequencies of 20-30 Hz, consistent with the system operating within this plastic range of contractility. Temperature was also a key factor in muscle contractility, as force was enhanced at lower temperatures and dramatically reduced with increasing temperatures Pharmacol. and genetic manipulations of critical components of Ca2+ regulation in both pre- and postsynaptic compartments affected the strength and time course of muscle contractions. A screen for modulators of muscle contractility led to identification and characterization of the mol. and cellular pathway by which the FMRFa peptide, TPAEDFMRFa, increases muscle performance. These findings indicate Drosophila NMJs provide a robust system to correlate synaptic dysfunction, regulation and modulation to alterations in excitation-contraction coupling. Key points : Larval muscle contraction force increases with stimulation frequency and duration, revealing substantial plasticity between 5 and 40 Hz. Fictive contraction recordings demonstrate endogenous motoneuron burst frequencies consistent with the neuromuscular system operating within the range of greatest plasticity. Genetic and pharmacol. manipulations of critical components of pre- and postsynaptic Ca2+ regulation significantly affect the strength and time course of muscle contractions. A screen for modulators of the excitation-contraction machinery identified a FMRFa peptide, TPAEDFMRFa and its associated signalling pathway, that dramatically increases muscle performance. Drosophila serves as an excellent model for dissecting components of the excitation-contraction coupling machinery.

Journal of Physiology (Oxford, United Kingdom) published new progress about Actins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

S’ari, Mark published the artcileLow dose scanning transmission electron microscopy of organic crystals by scanning moire fringes, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is STEM scanning moire fringes organic crystals; Bright field STEM; Dose-limited resolution; Low dose; Organic crystals; Scanning moiré fringes.

In the pharmaceutical industry, it is important to determine the effects of crystallization and processes, such as milling, on the generation of crystalline defects in formulated products. Conventional transmission electron microscopy and scanning transmission electron microscopy (STEM) can be used to obtain information on length scales unobtainable by other techniques, however, organic crystals are extremely susceptible to electron beam damage. This work demonstrates a bright field (BF) STEM method that can increase the information content per unit specimen damage by the use of scanning moire fringes (SMFs). SMF imaging essentially provides a magnification of the crystal lattice through the interference between closely aligned lattice fringes and a scanning lattice of similar spacing. The generation of SMFs is shown for three different organic crystals with varying electron beam sensitivity, theophylline, furosemide and felodipine. The electron fluence used to acquire the BF-STEM for the most sensitive material, felodipine was approx. 3.5 e-/Å2. After one addnl. scan of felodipine (total fluence of approx. 7.0 e-/Å2), the SMFs were no longer visible due to extensive damage caused to the crystal. Irregularity in the SMFs suggested the presence of defects in all the organic crystals. Further effort is required to improve the data anal. and interpretation of the resulting SMF images, allowing more information regarding the crystal structure and defects to be extracted

Micron published new progress about Crocidolite asbestos Role: ANT (Analyte), ANST (Analytical Study). 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