Category: 21829-25-4

Albrizio, Maria published the artcileThe role of bicarbonate in the modulation of capacitation, spontaneous acrosome reaction and motility of equine fresh and frozen spermatozoa, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Theriogenology (2022), 112-118, database is CAplus and MEDLINE.

In this study, we defined the composition of the culture medium that yield a significant percentage of alive and functional equine spermatozoa during enough time before artificial insemination. The effects of sodium bicarbonate were analyzed in fresh and frozen semen in respect to sperm viability, capacitation, spontaneous acrosome reaction and several kinetic parameters such as total motility, progressive motility, VCL, VSL, ALH, BCF, LIN. Moreover, employing Bayk-6844 and Nifedipine, the involvement of L-type voltage-gated calcium channels in the modulation of intracellular calcium concentrations was investigated. Results evidenced an immediate effect of sodium bicarbonate in reducing fresh sperm viability and in increasing capacitation and spontaneous acrosome reaction of fresh and frozen spermatozoa. Furthermore, it affected total and progressive motility of fresh and frozen semen. Because of the sudden effects of the compound, we think that a buffer lacking sodium bicarbonate is more suitable to preserve the viability and the functional state of equine spermatozoa required to undergo at the right time those modifications necessary for fertilization. We also demonstrated that intracellular calcium modifications induced by Bayk-8644 and Nifedipine are not involved in signals related to vitality, capacitation, spontaneous acrosome reaction and motility.

Theriogenology 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

Peng, De-wei published the artcileConnexin 43 participates in atrial electrical remodelling through colocalization with calcium channels in atrial myocytes, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Clinical and Experimental Pharmacology and Physiology (2022), 49(1), 25-34, database is CAplus and MEDLINE.

Atrial fibrillation (AF) is associated with atrial conduction disturbances caused by elec. and/or structural remodelling. In the present study, author hypothesized that connexin might interact with the calcium channel through forming a protein complex and, then, participates in the pathogenesis of AF. Western blot and whole-cell patch clamp showed that protein levels of Cav1.2 and connexin 43 (Cx43) and basal ICa,L were decreased in AF subjects compared to sinus rhythm (SR) controls. In cultured atrium-derived myocytes (HL-1 cells), knocking-down of Cx43 or incubation with 30 mmol/L glycyrrhetinic acid significantly inhibited protein levels of Cav1.2 and Cav3.1 and the c.d. of I_Ca,L and I_Ca,T. Incubation with nifedipine or mibefradil decreased the protein level of Cx43 in HL-1 cells. Moreover, Cx43 was colocalized with Cav1.2 and Cav3.1 in atrial myocytes. Therefore, Cx43 might regulate the I_Ca,L and I_Ca,T through colocalization with calcium channel subunits in atrial myocytes, representing a potential pathogenic mechanism in AF.

Clinical and Experimental Pharmacology and Physiology 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, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Abdallah el hadj, A. published the artcileAI-PCSAFT approach: New high predictive method for estimating PC-SAFT pure component properties and phase equilibria parameters, Product Details of C17H18N2O6, the publication is Fluid Phase Equilibria (2022), 113297, database is CAplus.

In this work, a new approach based on the association of Artificial intelligence method (AI) and PC-SAFT equation of state is applied to conceive a model for estimating the solubility of solid drugs in supercritical carbon dioxide. Neuro-equation of state approach (NES) is the new technique that takes benefit from the advantages of both ANN and PC-SAFT equation of state. The new method decomposes into three main stages, first the optimization of direct ANN for predicting solids-scCO₂ phase equilibrium (where 15 binary systems are used), then the ANN inverse is performed to be an alternative to group contribution methods (GCMs) for estimating the pure components and phys. properties (reduce the uncertainty committed in estimating these properties) and enhance the PCSAFT equation of state to estimate phase equilibrium parameters and finally, ANN-PCSAFT approach is used to estimate the solubility of 213 solid solutes in supercritical carbon dioxide. The performance strategy has been carried out using a linear regression anal. of the predicted vs. exptl. outputs, as an indication of the predictive ability of the developed method. The new approach is successfully applied to the phase equilibrium modeling for 213 binary systems with high accuracy (the comparison in terms of average absolute relative deviation (AARD %) showed a variation from 2 to 6%) and allowed to enhance the phase equilibrium modeling by reducing the number of optimized parameters and surpass the main drawbacks faced in this area mainly the non-availability of phys. properties and EOS pure component properties and the limitation of the equation of state.

Fluid Phase Equilibria 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

Liang, Ling published the artcileComparative peripheral edema for dihydropyridines calcium channel blockers treatment: A systematic review and network meta-analysis, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Clinical Hypertension (Hoboken, NJ, United States) (2022), 24(5), 536-554, database is CAplus and MEDLINE.

Dihydropyridine calcium channel blockers (DHPCCBs) are widely used to treat hypertension and chronic coronary artery disease. One common adverse effect of DHPCCBs is peripheral edema, particularly of the lower limbs. The side effect could lead to dose reduction or discontinuation of the medication. The combination of DHPCCBs and renin-angiotensin system blockers has shown to reduce the risk of DHPCCBs-associated peripheral edema compared with DHPCCBs monotherapy. Author performed the current systematic review and network meta-anal. of randomized controlled trials (RCTs) to estimate the rate of peripheral edema with DHPCCBs as a class and with individual DHPCCBs and the ranking of the reduction of peripheral edema. The effects of renin-angiotensin system blockers on DHPCCBs network meta-anal. were created to analyze the ranking of the reduction of peripheral edema. A total of 3312 publications were identified and 71 studies with 56,283 patients were included. Nifedipine ranked highest in inducing peripheral edema (SUCRA 81.8%) and lacidipine (SUCRA 12.8%) ranked the least. All DHPCCBs except lacidipine resulted in higher relative risk (RR) of peripheral edema compared with placebo. Nifedipine plus angiotensin receptor blocker (SUCRA: 92.3%) did not mitigate peripheral edema and amlodipine plus angiotensin-converting enzyme inhibitors (SUCRA: 16%) reduced peripheral edema the most. Nifedipine ranked the highest and lacidipine ranked the lowest amongst DHPCCBs for developing peripheral edema when used for cardiovascular indications. The second or higher generation of DHPCCBs combination with ACEIs or ARBs or diuretics lowered the chance of peripheral edema development compared to single DHPCCB treatment.

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, 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

Engin, Seckin published the artcileThe inhibitory effect of trimetazidine on detrusor contractility – a potential repositioning of trimetazidine for the treatment of overactive bladder., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is The Journal of pharmacy and pharmacology (2022), 74(1), 94-102, database is MEDLINE.

OBJECTIVES: This study aimed to identify the effect of trimetazidine (TMZ), an antianginal drug, on detrusor smooth muscle (DSM) contractility and its possible mechanisms of action. METHODS: We performed in-vitro contractility studies on isolated mouse DSM strips and investigated the effect of TMZ on Ca2+ levels in fura-2-loaded A7r5 cells. KEY FINDINGS: TMZ (300 or 1000 µM) inhibited carbachol (CCh)- and KCl-induced contractions and produced a concentration-dependent (10-1000 µM) relaxation in KCl-precontracted DSM strips. TMZ-induced relaxation was markedly decreased by BaCl2, an inward-rectifying K+ channel blocker, but was not altered by preincubation with tetraethylammonium, glibenclamide, 4-aminopyridine, propranolol, L-NAME or methylene blue. TMZ (300 or 1000 µM) reduced both the CaCl2-induced contraction of depolarized DSM strips under Ca2+-free conditions and the CCh-induced contraction of DSM strips preincubated with nifedipine in Ca2+-containing Krebs solution. Furthermore, TMZ (1000 µM) significantly decreased the Ca2+ levels in fura-2-loaded A7r5 cells. CONCLUSIONS: TMZ decreased DSM contractility and caused a concentration-dependent relaxation of the tissue possibly through its actions on Ca2+ transients and K+ channels. Our results provide preclinical evidence that TMZ would be a potential candidate to treat disorders related to the overactivity of the bladder.

The Journal of pharmacy and pharmacology 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

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