Month: December 2022

Zadymova, N. M. published the artcileNanoemulsions Containing Incorporated Lipophilic Drug, Felodipine, and Microheterogeneous Adhesive Polymer Matrices Based on These Nanoemulsions, SDS of cas: 72509-76-3, the main research area is lipophilic felodipine microheterogeneous adhesive polymer matrix nanoemulsion.

Oil-in-water nanoemulsions (NEs) have been obtained with a simple composition, in which a lipophilic non-micelle-forming nonionic surfactant (Tween 85) serves as both a dispersed phase and a stabilizer. The NEs remain in a metastable state for a long time (several months) and have a highly developed sp. surface area (Ssp ≃ 63 m2/g) and a high solubilization capacity with respect to a lipophilic hypotensive drug, felodipine (FD). Nanosized droplets (dav ≃ 95 nm) of the NEs efficiently transport FD in an aqueous medium. The oil-in-water NEs of Tween 85 with incorporated FD and a solution of a polymer adhesive (a blend of polyisobutylenes having different mol. weights and polybutene) in heptane have been used to obtain oil1/water/oil2 double emulsions, which are used as premixes for polymer microheterogeneous matrixes. Obtained polymer films are characterized by a good adhesion to skin, the absence of FD crystallization, and a constant rate of its release for several hours.

Colloid Journal published new progress about Aggregation. 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

Sardesai, Mrunmayi published the artcileEngineering of Nanospheres Dispersed Microneedle System for Antihypertensive Action, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is engineering nanosphere microneedle system antihypertension; Hypertension; diltiazem; microneedles; nanospheres; nifedipine; vasodilator.

Background: A combinational therapy is mostly preferred in hypertension treatment because of low-dose and less side effects like pretibial edema, and gastrointestinal bleeding. Objective: So the objective of the present work was to formulate an advanced drug delivery system in the form of bio-responsive microneedles by incorporating nifedipine, a cardiodepressant and diltiazem, a vasodilator for effective synergism in the treatment of hypertension. Methods: The pH-responsive PLGA nanospheres of diltiazem were formulated using Water-in-Oil-in- Water (W/O/W) double emulsion and solvent-diffusion-evaporation technique. These nanospheres were added to nifedipine-PVP mixture and then incorporated into mold to develop microneedles. Results: The microneedles showed the release of nifedipine almost 96.93± 2.31% for 24 h due to high PVP solubilization. The nanospheres of diltiazem on contact with acidic pH of skin managed to form of CO2 bubbles and increase the internal pressure to burst PLGA shell due to pore formation. The mean blood pressure observed for the normal group was 89.58 ± 3.603 mmHg, whereas the treatment with the new formulation significantly reduced the mean blood pressure up to 84.11 ± 2.98 mmHg in comparison to the disease control group (109.9 ± 1.825 mm Hg). Conclusion: This system co-delivers the drugs nifedipine and diltiazem in hypertension and shows an advance alternative approach over conventional drug delivery system.

Current Drug Delivery published new progress about Aggregation. 21829-25-4 belongs to class pyridine-derivatives, 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:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Guo, Changchuan published the artcileTargeted and nontargeted screening and identification of 50 antihypertensive adulterants in dietary supplements and herbal medicines using quadrupole-orbitrap high resolution mass spectrometry with compound database, Category: pyridine-derivatives, the main research area is antihypertensive dietary supplement adulterant screening spectrometry; adulteration; antihypertensives; identification; mass spectrometry; orbitrap; traditional Chinese medicine.

In the present work, a novel database of drug compounds and a rapid screening method based on ultra-high performance liquid chromatog. coupled to high resolution orbitrap mass spectrometry were developed and applied in the screening and identification of targeted and nontargeted antihypertensive adulterants in dietary supplements and herbal medicines. The established screening database includes retention time, exact mass, fragments, isotopic pattern, and MS2 spectra library of the target compounds and thus provides automated search and identification of the targets with a single injection. The nontargeted compounds in the samples are identified through the full MS scan and MS2 data by using the Chemspider database and the data anal. in XCalibur, MassFrontier and TraceFinder software. In addition, this method possesses excellent quant. capacity. The novel approach was applied to 65 batches of samples that are claimed as “”all-natural”” products having the antihypertensive function, among which nine batches were found to be pos. Multiple targeted and nontargeted antihypertensive adulterants were detected at levels ranging from 2.8 to 27.9 mg/g. The novel database and screening method demonstrated herein will be promising and powerful tools for rapid screening of antihypertensive adulterants in dietary supplements and herbal medicines.

Journal of Separation Science published new progress about Adulterants. 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

Zhang, Shuo published the artcileCalcium plays a double-edged role in modulating cadmium uptake and translocation in rice, Application In Synthesis of 21829-25-4, the main research area is Oryza grain nifedipine calcium cadmium NRAMP1 translocation seedling; cadmium; calcium; crop safety; membrane transport; net Cd2+ influx; root-to-shoot translocation.

Cadmium (Cd) contamination in soils poses great risks to both agricultural production and human health. Calcium (Ca) is an essential element playing a significant role in protecting plants against Cd toxicity. However, how Ca affects Cd uptake and translocation in rice is still not fully elucidated. In this study, the regulatory role of Ca in Cd uptake and upward translocation was investigated in rice at different growth stages. Our results showed that the supplement of 5 mM Ca significantly reduced Cd uptake by rice roots, because of their competition for Ca-permeable channels as an absorption site and Ca-induced downregulation of OsNRAMP1 and OsNRAMP5. However, Ca application facilitated the upward translocation of Cd by both upregulating OsHMA2 to induce xylem loading of Cd and downregulating OsHMA3 to reduce vacuolar sequestration of Cd. Such contrary results suggested a double-edged role of Ca in regulating root Cd uptake and root-to-shoot Cd translocation in rice. Although it increased Cd content in the aboveground vegetative tissues during the whole growth period, the addition of 5 mM Ca eventually decreased Cd content in rice grains at the ripening stage. All these results suggest that Ca-based amendments possess great potential for the production of low-Cd rice grains.

International Journal of Molecular Sciences published new progress about Oryza sativa. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Charushin, Valery N. published the artcileRing transformations in reactions of heterocyclic compounds with nucleophiles. Part 26. 1,3- and 1,4-Cyclo adducts as intermediates in the pyrimidine to pyridine ring transformation of 5-nitropyrimidines by α-phenylacetamidines, Formula: C9H11N3O3, the main research area is pyrimidine reaction nucleophile; acetamidine phenyl reaction pyrimidine; pyridine amino nitropyrimidine.

5-Nitropyrimidine reacts with PhCH2CR:NH (R = NH2, NMe2, NEt2) at -40° to form σ adducts at the C-2 position of the ring, but gives 2-aminopyridine derivatives I at temperatures above 0 °. Experiments with 15N-labeled PhCH2C(:NH)NH2 showed that the reaction proceeds via different reaction pathways with replacement of either the N(1)-C(2)-N(3) or N(1)-C(2) fragment of the pyrimidine ring by the C-C-N or the C-C moiety of the amidine. The role of 1,3- and 1,4-cycloadducts as possible intermediates in the ring-transformation reaction is discussed.

Journal of Organic Chemistry published new progress about Nucleophiles. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Formula: C9H11N3O3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ngadjui, Esther published the artcileUterotonic Effects of Aqueous and Methanolic Extracts of Lannea acida in Wistar Rats: An In Vitro Study, Product Details of C17H18N2O6, the main research area is Lannea atosiban atropine nifedipine uterine contraction uterotonic; Calcium; In vitro; Lannea acida; Rats; Uterine contraction.

Lannea acida (Anacardiaceae), commonly called Kikie in the Noun division (West-Cameroon), is a tree whose bark is used locally to facilitate delivery. This study was aimed at evaluating the in vitro uterotonic effects of aqueous and methanol extracts of L. acida in Wistar rats. Uterine strips isolated from rats pretreated with 5μg estradiol (48 h) were mounted in a single-organ bath containing aerated and thermostated De Jalon solution (37°C). After equilibration, non-cumulative effects of L. acida extracts were recorded after application. The effect of the methanol extract (the most active extract) was monitored in the presence of atosiban (a competitive antagonist of oxytocin receptors), atropine (a specific type 3 muscarinic receptor antagonist), nifedipine (an L-type calcium channel antagonist), and 2-Aminoethoxydiphenyl borate (2-ADB, a specific antagonist of inositol 1,4,5-triphosphate receptors type 1), and in calcium-free medium containing EGTA to elucidate its mechanism of action. L. acida induced uterine contraction in a concentration-dependent manner with the methanol extract (1.506 ± 0.032 gf) being the most effective. Administration of atosiban (2μmol/L) and atropine (1μmol/L) reduced the contractile effect of L. acida. Complete inhibition was observed with nifedipine, 2-APB, and calcium-free medium containing EGTA. These results suggest that L. acida possesses uterotonic effects mediated through oxytocin receptors with mobilization of extracellular calcium.

Reproductive Sciences published new progress about Lannea acida. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Abduljalil, Khaled published the artcilePrediction of maternal pharmacokinetics using physiologically based pharmacokinetic models: assessing the impact of the longitudinal changes in the activity of CYP1A2, CYP2D6 and CYP3A4 enzymes during pregnancy, Application In Synthesis of 21829-25-4, the main research area is metabolizing CYP1A2 CYP2D6 CYP3A4 impact pregnancy; CYP1A2; CYP2D6; CYP3A4; Inter-individual variability; PBPK; Pharmacokinetics; Pregnancy.

Concerns over gestational effects on the disposition of drugs has highlighted the need for a better understanding of drug distribution and elimination during pregnancy. This study aimed at predicting maternal drug kinetics using a physiol. based pharmacokinetic (PBPK) modeling approach focusing on the observed gestational changes in three important Cytochrome P 450 metabolizing enzymes, namely, CYP1A2, CYP2D6 and CYP3A4 at different gestational weeks (GWs). The Pregnancy PBPK model within the Simcyp Simulator V19 was used to predict the pharmacokinetics of sensitive probes to these enzymes; namely caffeine, theophylline, metoprolol, propranolol, paroxetine, midazolam, nifedipine and rilpivirine. PBPK model predictions were compared against clin. data collated from multiple studies for each compound to cover a wide spectrum of gestational ages. Pregnancy PBPK model predictions were within 2-fold error and indicated that CYP1A2 activity is approx. 0.70, 0.44 and 0.30 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. On the other hand, CYP2D6 activity increases by 1.36, 2.16 and 3.10 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. Likewise, CYP3A4 activity increases by 1.25, 1.75 and 2.32 fold of the non-pregnant level at the end of the first, second and third trimesters, resp. The enzymes activity have been qualified throughout pregnancy. Quantified changes in drug dosing are most relevant during the third trimester, especially for drugs that are mainly eliminated by CYP1A2, CYP2D6 and CYP3A4 enzymes. The provided functions describing the continuous changes to the activity of these enzymes during pregnancy are important when modeling long term pharmacokinetic studies where longitudinal modeling or time-varying covariates are used.

Journal of Pharmacokinetics and Pharmacodynamics published new progress about Homo sapiens. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jin, Cheng Hua published the artcileSynthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors, Related Products of pyridine-derivatives, the main research area is ALK5 inhibition triazolopyridinylpyrazole pyridinyl preparation.

A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. 4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-N-(4-methoxyphenyl)-3-(6-methylpyridin-2-yl)-1H-pyrazole-1-carbothioamide (I) inhibited ALK5 phosphorylation with IC50 value of 0.57 nM and showed 94% inhibition at 100 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.

Bioorganic & Medicinal Chemistry Letters published new progress about Homo sapiens. 614750-81-1 belongs to class pyridine-derivatives, name is [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, and the molecular formula is C7H5N3O, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Sidhu, Preetpal S. published the artcileDevelopment of Novel Vitamin D Receptor-Coactivator Inhibitors, Safety of 2-Methoxynicotinaldehyde, the main research area is novel vitamin D receptor coactivator inhibitor; 3-indolylmethanamines; CAMP; CYP24A1; HL60; VDR; Vitamin D receptor; apoptosis; fluorescence polarization; high throughput screening; steroid receptor coactivator.

Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation, and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves like a VDR antagonist by repressing 1,25-(OH)2D3 activated gene transcription. In addition, PS121912 induced apoptosis in HL-60.

ACS Medicinal Chemistry Letters published new progress about Homo sapiens. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Safety of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Krollik, Katharina published the artcileThe effect of buffer species on biorelevant dissolution and precipitation assays – Comparison of phosphate and bicarbonate buffer, SDS of cas: 72509-76-3, the main research area is carbamazepine probenecid griseofulvin phosphate bicarbonate buffer; Bicarbonate buffer; Biorelevant media; Dissolution; Precipitation; Solubility testing.

Biorelevant solubility and dissolution testing is an important tool during pharmaceutical development, however, solubility experiments performed using biorelevant media often do not properly match the solubility data observed in human intestinal fluids. Even though the bicarbonate buffer is the predominant buffer system in the small intestine, in vitro assays are commonly performed using non-volatile buffer systems like phosphate and maleate. In the current study, bicarbonate- and phosphate-buffered biorelevant media were applied to solubility, dissolution, and precipitation testing for a broad range of model compounds It was found that the medium affects primarily the dissolution kinetics. However, with the knowledge of the unique buffering properties of bicarbonate buffer in the diffusion layer, it was not always possible to predict the effect of buffer species on solubility and dissolution when changing from phosphate to bicarbonate buffer. This once again highlights the special role of bicarbonate buffer for simulating the conditions in the human intestinal fluids. Moreover, it is necessary to further investigate the factors which may cause the differences in solubility and dissolution behavior when using phosphate- vs. bicarbonate-buffered biorelevant media.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Homo sapiens. 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