Tag: M.W=300-350

Schneider, D. published the artcileInfluence of 3 antivertiginous medications on the vigilance of healthy volunteers, Product Details of C10H20N2O6S2, the publication is International Journal of Clinical Pharmacology and Therapeutics (2003), 41(4), 171-181, database is CAplus and MEDLINE.

In the present randomized, comparative, double-blind, 3-way crossover study, possible effects of 3 antivertiginous medications on vigilance were investigated. Thirty healthy volunteers received single doses of a fixed combination of cinnarizine 20 mg and dimenhydrinate 40 mg (Arlevert, ARL), dimenhydrinate 50 mg, or betahistine dimesylate 12 mg, in randomized order at 1-wk intervals. Spontaneous brain elec. activity (EEG), acoustic late evoked potentials (ALEP) with P300, and reaction time were measured before and 90 (t₉₀) and 180 min (t₁₈₀) after drug intake. All 3 medications led to a delay of P300 (primary criterion) and a decrease of its amplitude. The maximum delay at t₁₈₀ was found for dimenhydrinate (16.42 ms) and the lowest for betahistine (6.33 ms). The differences in ARL vs. dimenhydrinate and ARL vs. betahistine were not statistically significant (p > 0.05). Spectral anal. of spontaneous EEG showed slight and similar decreases in the power in the α-band under dimenhydrinate and ARL (p = 0.07 and p = 0.03 with respect to baseline, resp.), but basically no change under betahistine. There was no effect on reaction time by either medication. None of the subjects reported drowsiness or any other adverse event. The findings confirm the reported suitability of P300 latency for measurement of drug effects on brain activity, but provide no indication of concomitant impairment of performance capacity by the tested drugs. Global assessment of the results suggests that the fixed combination cinnarizine 20 mg/dimenhydrinate 40 mg exerts only a minor effect on vigilance, not significantly different from betahistine, which is commonly regarded as a non-sedating antivertiginous drug.

International Journal of Clinical Pharmacology and Therapeutics 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

Okamura, H. published the artcileEcotoxicity of the degradation products of triphenylborane pyridine (TPBP) antifouling agent, Category: pyridine-derivatives, the publication is Chemosphere (2009), 74(9), 1275-1278, database is CAplus and MEDLINE.

Triphenylborane pyridine (TPBP) is an alternative to organotin antifouling compounds This work aimed to identify the unknown Peak #1, and to evaluate the ecotoxicity of TPBP and its degradation products. Peak #1 was produced from TPBP dissolved in acetonitrile under UV-A photolysis using a high-pressure Hg lamp. The Peak #1 fraction was purified using 2-step column chromatog. from a TPBP-acetonitrile solution The major compound of the fraction was identified as being biphenyl from the ¹H NMR and ¹³C NMR spectra. The ecotoxicity of 4 degradation products (diphenylborane hydroxide, phenylborane dihydroxide, phenol, and biphenyl) and TPBP towards 2 marine planktons were assessed. The 48 h LC₅₀ values of the crustacean, Artemia salina, were 0.13 mg L^-1 for TPBP, 14 mg L^-1 for biphenyl, 17 mg L^-1 for phenol, and >50 mg L^-1 for the other degradation products. The 72 h EC₅₀ values of the diatom, Skeletonema costatum, were 0.0022 mg L^-1 for TPBP, 1.2 mg L^-1 for biphenyl, and >2 mg L^-1 for the other degradation products. Thus, the ecotoxicity of biphenyl and the other degradation products were not high compared to the parent compound, TPBP.

Chemosphere 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, Category: pyridine-derivatives.

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

Shahar, Or David published the artcileA high-throughput chemical screen with FDA approved drugs reveals that the antihypertensive drug Spironolactone impairs cancer cell survival by inhibiting homology directed repair, Application In Synthesis of 54856-23-4, the publication is Nucleic Acids Research (2014), 42(9), 5689-5701, database is CAplus and MEDLINE.

DNA double-strand breaks (DSBs) are the most severe type of DNA damage. DSBs are repaired by non-homologous end-joining or homol. directed repair (HDR). Identifying novel small mols. that affect HDR is of great importance both for research use and therapy. Mols. that elevate HDR may improve gene targeting, whereas inhibiting mols. can be used for chemotherapy, since some of the cancers are more sensitive to repair impairment. Here, the authors performed a high-throughput chem. screen for FDA approved drugs, which affect HDR in cancer cells. The authors found that HDR frequencies are increased by retinoic acid and Idoxuridine and reduced by the antihypertensive drug Spironolactone. The authors further revealed that Spironolactone impairs Rad51 foci formation, sensitizes cancer cells to DNA damaging agents, to Poly (ADP-ribose) polymerase (PARP) inhibitors and crosslinking agents and inhibits tumor growth in xenografts, in mice. This study suggests Spironolactone as a new candidate for chemotherapy.

Nucleic Acids Research 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 C18H12ClNO, Application In Synthesis of 54856-23-4.

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

Chen, Jinghu published the artcileFacile synthesis of highly porous hyper-cross-linked polymer for light hydrocarbon separation, HPLC of Formula: 971-66-4, the publication is Polymer Engineering & Science (2021), 61(3), 662-668, database is CAplus.

Light hydrocarbon separation is a crucial process associated with high energy expenditure in the petrochem. industry. The utilization of porous organic materials as solid porous adsorbents for light hydrocarbon separation has found widespread attention because of the advantages of low cost, excellent stability, and good recyclability. Here, we present the facile synthesis of a porous organic material, constructed from pyridine-triphenylborane by using a Friedel-Crafts alkylation coupling reaction, affording the hyper-crosslinked polymer, HCP-B. HCP-B features significant thermal stability, and high surface area. Gas adsorption experiments show that this material adsorbs much larger amounts of ethane, ethylene, and acetylene than that of methane. Ideal adsorbed solution theory (IAST) calculations also predict that HCP-B selectively adsorbs ethane, ethylene, and acetylene over methane. Both are indicative of the great potential of HCP-B in light hydrocarbon separation

Polymer Engineering & Science 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, HPLC of Formula: 971-66-4.

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

Gui, Yue published the artcileCrystal Energy Landscape of Nifedipine by Experiment and Computer Prediction, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Crystal Growth & Design (2022), 22(2), 1365-1370, database is CAplus.

The six polymorphs of nifedipine (NIF) known at present have been discovered over the past 50 years, and the most recent one (δ), discovered in 2020, came from an unusual route. This polymorph is ranked second in thermodn. stability but evaded all previous workers until its melt was seeded with the crystal of a foreign substance, felodipine, in which the mol. has a different conformation from all other NIF polymorphs known at that time. Given this unusual discovery in the lab, we investigated whether crystal structure prediction (CSP) can find this and other polymorphs in a “routine” search. We show that our CSP finds all ordered polymorphs of NIF known at present as low-energy structures (Ranks 1, 3, 4, and 43), including the most recent one unveiled by pseudoseeding (Rank 4). NIF being a flexible mol., it is of interest to learn which of its many conformers provides the best building block for crystals. An exptl. investigation of this question is limited by survival; i.e., information exists on the structures that are observed but not on those that are difficult to observe or not yet discovered. In this regard, our “computer experiments” access the full range of possibilities. We find that the synperiplanar (sp) conformer with respect to Ph torsion produces lower-energy crystals than the antiperiplanar (ap) conformer, with the most stable ap crystal being 4 kJ/mol higher in energy than the most stable sp structure. Exptl., the sp conformer dominates the ap in solution and is the only conformer observed in crystals. With respect to the ester torsions, the cis/trans conformer produces the lowest-energy crystals, followed by the cis/cis conformer and by the trans/trans conformer. Exptl., five of the six known polymorphs contain the cis/trans conformer, one contains the cis/cis conformer, and none contain the trans/trans conformer. Overall, the CSP is remarkably successful in predicting the polymorphs of NIF in spite of its complex conformational space and provides a quant. assessment of the relative costs of employing different conformers as units of crystal building.

Crystal Growth & Design 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, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Jung, Ju young published the artcileEnhanced Solubility Through Particle Size Control, Modification of Crystal Behavior, and Crystalline Form Changes in Solid Dispersion of Nifedipine, Related Products of pyridine-derivatives, the publication is Biotechnology and Bioprocess Engineering (2022), 27(1), 105-110, database is CAplus.

The purpose of this study was to investigate the selectivity of polymers and the suitability of spray drying to enhance nifedipine solubility Nifedipine alone or in combination with polymers was dissolved in a mixed solvent of methylene chloride and ethanol. The hydrophilic polymers used were PVP K-30, HPMC, HPMCP, Eudragit, and HPMCAS. Each solid dispersion was prepared using a laboratory spray dryer. The spray-dried solid dispersants were characterized by SEM, DSC, and XRPD anal., and dissolution tests compared the dissolution rates of nifedipine solid dispersants and nifedipine. The results showed that all spray-dried solid dispersions were in an amorphous form. Dissolution tests were performed at pH 1.2 (artificial gastric juice) and pH 6.8 (artificial intestinal juice) to evaluate solid dispersion solubility The solid dispersion containing HPMC showed a notably enhanced dissolution rate under both pH conditions. Interestingly, HPMCP and HPMCAS showed almost no enhancement of dissolution behavior at pH 1.2, but a significant increase (10 times or higher) over that of the pure polymer at pH 6.8. Solubility enhancement of poorly soluble drugs differs markedly among the polymers used for spray drying. From the results, HPMCP and HPMCAS are suitable as carriers for drugs with poor solubility that require acid resistance.

Biotechnology and Bioprocess Engineering 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

Gui, Yue published the artcilePolymorphic selectivity in crystal nucleation, SDS of cas: 21829-25-4, the publication is Journal of Chemical Physics (2022), 156(14), 144504, database is CAplus and MEDLINE.

Crystal nucleation rates were measured in the supercooled melts of 2 richly polymorphic glass-forming liquids: 5-Me-2-[(2-nitrophenyl)amino]-3-thiophenecarbonitrile (ROY) and nifedipine (NIF). ROY is known for its crystals of red, orange, and yellow colors and many polymorphs of solved structures. Of the many polymorphs, ON (orange needles) nucleates the fastest with the runner up (Y04) trailing by a factor of 10³ when compared under the same mobility-limited condition, while the other unobsd. polymorphs are slower yet by â‰? orders of magnitude. Of the 6 polymorphs of NIF, γ’ nucleates the fastest, β’ is slower by a factor of 10, and the rest are slower yet by â‰? decades. In both systems, the faster-nucleating polymorphs are not built from the lowest-energy conformers, while they tend to have higher energies and lower densities and thus greater similarity to the liquid phase by these measures. The temperature ranges of this study covered the glass transition temperature T_g of each system, and no evidence that the nucleation rate is sensitive to the passage of T_g were found. At the lowest temperatures studied, the rates of nucleation and growth are proportional to each other, indicating that a similar kinetic barrier controls both processes. The classical nucleation theory provides an accurate description of the observed nucleation rates if the crystal growth rate is used to describe the kinetic barrier for nucleation. The quant. rates of both nucleation and growth for the competing polymorphs enable prediction of the overall rate of crystallization and its polymorphic outcome. (c) 2022 American Institute of Physics.

Journal of Chemical Physics 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, SDS of cas: 21829-25-4.

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

Lee, Hao-Wei published the artcileComparative efficacy of generic nifedipine versus brand-name amlodipine for hypertension management in Taiwan, Product Details of C17H18N2O6, the publication is Journal of Clinical Hypertension (Hoboken, NJ, United States) (2022), 24(7), 870-877, database is CAplus and MEDLINE.

The control rate of hypertension remains concerning, indicating the requirement for better management strategies. The calcium channel blockers brand-name amlodipine and nifedipine with extended-release formulations demonstrate similar clin. efficacy. However, the efficacy of generic nifedipine remains obscure. We compared the efficacy of generic nifedipine and brand-name amlodipine in terms of cardiovascular (CV) outcomes. Patients prescribed generic nifedipine (SRFC CYH) or brand-name amlodipine besylate (Norvasc, Pfizer) between August 1, 2017, and July 31, 2018, were enrolled; patients with CV events within 3 mo were excluded. CV outcomes included CV death, nonfatal myocardial infarction (MI), nonfatal ischemic stroke, hospitalization for heart failure, and composite endpoints of 3P- and 4P-major adverse cardiac events (MACE). A total of 1625 patients treated with nifedipine (SRFC CYH) and 16 587 patients treated with Norvasc were included. After propensity score matching, there were 995 and 4975 patients in the nifedipine CYH and Norvasc groups, resp. At a mean follow-up period of 30.3 ± 6.4 mo, nifedipine CYH was comparable to Norvasc in terms of CV death (P = .107), nonfatal MI (P = .121), nonfatal ischemic stroke (P = .453), hospitalization for heart failure (P = .330), 3P-MACE (P = .584), and 4P-MACE (P = .274). Cox regression anal. revealed that nifedipine CYH and Norvasc had similar efficacy in terms of 3P-MACE (hazard ratio, 0.970; 95% confidence interval, 0.601-1.565, P = .900) and 4P-MACE (hazard ratio, 0.880; 95% confidence interval, 0.628-1.233, P = .459). In conclusion, Nifedipine SRFC CYH and Norvasc have comparable clin. efficacy for hypertension management.

Journal of Clinical Hypertension (Hoboken, NJ, United States) 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, Product Details of C17H18N2O6.

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

Wang, Xinyi published the artcileRapid screening of illegal additives in functional food using atmospheric pressure solids analysis probe coupled to a portable mass spectrometer, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Pharmaceutical and Biomedical Analysis (2022), 114722, database is CAplus and MEDLINE.

Pharmaceutical drugs like Sildenafil are illegally added to functional food such as nutritional supplements and herbal remedies to deliver drugs without a regular prescription to consumers. Rapid screening of illegal additives is desirable for the public security department. The seized samples are often large in number and unknown in composition; methods are needed for qual. screening of unknown samples. Here, a new approach is presented based on atm. pressure solids anal. probe (ASAP) coupled with single-quadrupole mass spectrometer to rapidly screen 42 common illegal additives in six categories of functional food. The ASAP-MS method could be applied to solid or liquid sample anal. with a very simple pre-treatment and no LC chromatog. separation, using a home-built library; the identification of suspicious additives could be obtained rapidly. More importantly, the approach is sensitive enough for complex matrix samples like coffee samples. 21 batches of seized unknown samples were tested by the ASAP-MS, and the pos. results were confirmed by LC-MS/MS(QQQ), indicating that the ASAP-MS method is effective and reliable. The ASAP-MS with home-built library is a promising method for rapid screening of illegal additives in functional food, which could be widely used in the grassroots police station that lack professional laboratory environment.

Journal of Pharmaceutical and Biomedical Analysis 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 C9H8BNO2, 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

Kim, Min Jun published the artcileHeme oxygenase-1 gene delivery for altering high mobility group box-1 protein in pancreatic islet, Synthetic Route of 21829-25-4, the publication is Journal of Controlled Release (2022), 326-337, database is CAplus and MEDLINE.

Pancreatic islet transplantation is a promising strategy for the treatment of type I diabetes. High-mobility group box-1 (HMGB1), highly expressed in islet cells, is a potent immune stimulator in immune rejection. Heme oxygenase-1 (HO1) gene therapy can modulate the release of HMGB1 by altering intracellular mols. for successful cell transplantation. After delivery of the heme oxygenase-1 (HO1) gene to islet cells using an adeno-associated viral vector (AAV), it was evaluated the changes in cytoplasmic Ca2+ ions and calcineurin activity as well as histone acetyltransferase (HAT) and Poly(ADP) ribose polymerase-1 (PARP-1). Inhibition of HMGB1 release was evaluated through altering these intracellular mols. Then, after transplantation of HO1-transduced islets, the therapeutic effect of them was evaluated through measuring blood glucose level to diabetic mice and through immunohistochem. anal. The transduced HO1 gene significantly inhibited HMGB1 release in islets that was under the cell damage by hypoxia exposure. It was confirmed that this result was initially due to the decrease in cytoplasmic Ca2+ ion concentration and calcineurin activity. In addition, the delivered HO1 gene simultaneously reduced the activity of HAT and PARP-1, which are involved in the translocation of HMGB1 from the nucleus to the cytoplasm. As a result, when the HO1 gene-transduced islets were transplanted into diabetic mice, the treatment efficiency of diabetes was effectively improved by increasing the survival rate of the islets. Collectively, these results suggest that HO1 gene transfer can be used for successful islet transplantation by altering the activity of intracellular signal mols. and reducing HMGB1 release.

Journal of Controlled Release 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, Synthetic Route of 21829-25-4.

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