Category: 21829-25-4

Fu, Chengxiao published the artcilePopulation Pharmacokinetic Modelling for Nifedipine to Evaluate the Effect of Parathyroid Hormone on CYP3A in Patients with Chronic Kidney Disease., Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Drug design, development and therapy (2022), 2261-2274, database is MEDLINE.

Purpose: Parathyroid hormone (PTH) can induce the downregulation of CYP3A in chronic kidney disease (CKD). Nevertheless, the effect of PTH on CYP3A-mediated clearance pathways from a clinical perspective remains unclear. Methods: This study employed population pharmacokinetic (PopPK) modeling to delineate potential changes in CYP3A activity in patients with CKD. Pharmacokinetic data for nifedipine, a typical CYP3A substrate, as well as covariate information, were prospectively collected from 157 patients with a total of 612 concentrations. PopPK data analysis was performed using a nonlinear mixed-effects model. Results: The pharmacokinetics of nifedipine were optimally described according to a one-compartment model with zero-order absorption and first-order elimination. The estimated population parameters (and interindividual variability) were apparent clearance (CL/F) 49.61 L/h (58.33%) and apparent volume of distribution (V/F) 2300.26 L (45.62%), and the PTH level negatively correlated with CL/F. In comparison with the reference level, it was observed that the dosage of nifedipine should be reduced with the maximum boundary value of PTH, after a Monte Carlo simulation. Conclusion: This study provides insight into the effects of PTH on CYP3A-mediated clearance pathways. Moreover, PTH could be used as a guide for the appropriate administration of CYP3A eliminated drugs in patients with CKD.

Drug design, development and therapy 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

Xiong, Zhihui published the artcileFour kinds of tocolytic therapy for preterm delivery: Systematic review and network meta-analysis, Formula: C17H18N2O6, the publication is Journal of Clinical Pharmacy and Therapeutics (2022), 47(7), 1036-1048, database is CAplus and MEDLINE.

Meta-anal. of premature birth affects more than 15 million infants, as well as mothers and families around the world. With the relaxation of the two-child policy, the problem of premature birth has become relatively prominent in China. According to statistics, China had a birth population of 15.23 million in 2018, with a considerably large number of premature births. This study aims to evaluate the efficacy and safety of tocolysis in the treatment of preterm delivery, provide clin. evidence for medical staff and promote the self-management of patients with premature births. Four English databases (PubMed, Embase, Cochrane Library and Web of Science) were retrieved by computer, the retrieval time was from the establishment of each database to Nov. 2021, and the randomized controlled trials for the treatment of preterm delivery were screened according to the pre-set natriuretic exclusion criteria. After literature screening, data selection and risk of bias evaluation were independently conducted by two researchers. R 4.1.1 and Stata 17.0 software were used for statistical anal. A total of 44 RCTs were included, including 6939 patients. The results of network meta-anal. reveal that in terms of effectiveness, indomethacin was the most effective intervention measure, followed by nifedipine, and the difference was statistically significant; regarding safety, nifedipine was the safest intervention measure, followed by indomethacin, and the difference was statistically significant; and in respect of adverse reactions, ritodrine had the highest probability, and the difference was statistically significant. Nifedipine may be better for delayed delivery and less likely to produce adverse pregnancy outcomes, followed by indomethacin. Limited by the number and quality of recipient studies, the aforementioned conclusions need to be verified through more high-quality studies. At the same time, the focus should be on patients with twin pregnancy and patients with clin. manifestations of extreme preterm delivery.

Journal of Clinical Pharmacy and Therapeutics 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 C7H13NO2, Formula: C17H18N2O6.

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

Oraebosi, M. I. published the artcileDiurnal efficacy of alpha-lipoic acid/nifedipine/glimepiride combination mitigates diabetic neuropathies in rats, HPLC of Formula: 21829-25-4, the publication is Annales Pharmaceutiques Francaises (2022), 80(3), 291-300, database is CAplus and MEDLINE.

Time-dependent effects of alpha-lipoic acid/nifedipine/glimepiride combination on diabetic neuropathies were investigated in rats. 7 groups (n = 9) of rats were used.First and second groups were apparently normal and diabetic rats resp., and were administered 1 mL/kg distilled water. The rest of the groups were diabetic and administered 10 mg/kg glimepiride at night-time (8:00 pm). Groups 4-7 were administered addnl. 20 mg/kg nifedipine at morning-time (8:00 am), while groups 5-7 were also administered 100 mg/kg alpha-lipoic acid (ALA) in the morning, afternoon and night-time resp. (8:00 am, 2:00 pm and 8:00 pm). During the 28 days of oral treatment, paw pressure, tail immersion and motor coordination tests were conducted. The rats were euthanized on the 29th day after a charcoal meal. The small intestines were excised to determine intestinal transit while the brain was collected, homogenised and used to determine levels of oxidative stress.Data show that treatment with ALA at 8:00 am or 2:00 pm significantly (P �0.01) produced a delay in the onset and improved prognosis of neuropathies. Treatment with ALA at 8:00 pm prevented manifestation of neuropathies throughout the study with pos. antioxidant effects.Time-dependent ALA treatment in combination with nifedipine and glimepiride should be studied in humans with an approx. similar circadian timing. This may provide addnl. clin. therapeutic options for diabetic neuropathies.

Annales Pharmaceutiques Francaises 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, HPLC of Formula: 21829-25-4.

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

Loh, Yean Chun published the artcileThe predominance of endothelium-derived relaxing factors and beta-adrenergic receptor pathways in strong vasorelaxation induced by 4-hydroxybenzaldehyde in the rat aorta, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Biomedicine & Pharmacotherapy (2022), 112905, database is CAplus and MEDLINE.

4-Hydroxybenzaldehyde (4HB), known as ρ-hydroxybenzaldehyde, is commonly present in traditional Chinese medicine herb, most frequently used for hypertension treatment. This research aims to determine the potency of 4HB’s vasorelaxant action. In the study, the vasodilation effect of 4HB was evaluated using in vitro isolated rat aortic rings assay. The aortic rings were pre-incubated with resp. antagonists before being pre-contracted with phenylephrine (PE) and challenged with various concentrations of 4HB for mechanistic action studies. R_max (maximal vasodilation) and pEC₅₀ (neg. logarithm of half-maximal effective concentration) values of each experiment were determined for comparison purposes. 4HB caused vasodilation on endothelium-intact aortic rings which pre-contracted with PE (pEC₅₀ = 3.53 ± 0.05, R_max = 100.95 ± 4.25%) or potassium chloride (pEC₅₀ = 2.96 ± 0.13, R_max = 72.13 ± 4.93%). The vasodilation effect of 4HB was significantly decreased in the absence of an endothelium (pEC₅₀ = 2.21 ± 0.25, R_max = 47.96 ± 4.16%). The atropine, 4-aminopyridine, Nω-nitro–arginine Me ester, glibenclamide, and propranolol significantly reduced the vasorelaxation effect of 4HB. Besides that, 4HB blocked the voltage-operated calcium channel (VOCC) and regulated the intracellular Ca²⁺ release from the sarcoplasmic reticulum (SR) in the aortic ring. Thus, the results indicated that 4HB exerted its vasodilatory effect via cGMP and β2 pathways, M₃-dependent PLC/IP₃ pathways, and potassium and calcium channels.

Biomedicine & Pharmacotherapy 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

van Winden, Tijn M S published the artcileTocolysis with nifedipine versus atosiban and perinatal outcome: an individual participant data meta-analysis., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is BMC pregnancy and childbirth (2022), 22(1), 567, database is MEDLINE.

BACKGROUND: Worldwide, nifedipine and atosiban are the two most commonly used tocolytic agents for the treatment of threatened preterm birth. The aim of this study was to evaluate the effectiveness of nifedipine and atosiban in an individual participant data meta-analysis (IPDMA). METHODS: We investigated the occurrence of adverse neonatal outcomes in women with threatened preterm birth by performing an IPDMA, and sought to identify possible subgroups in which one treatment may be preferred. We searched PubMed, Embase, and Cochrane for trials comparing nifedipine and atosiban for treatment of threatened preterm birth between 24^0/7 and 34^0/7 weeks’ gestational age. Primary outcome was a composite of perinatal mortality and neonatal morbidities including respiratory distress syndrome, intraventricular haemorrhage, periventricular leucomalacia, necrotising enterocolitis, and sepsis. Secondary outcomes included NICU admission, prolongation of pregnancy and GA at delivery. For studies that did not have the original databases available, metadata was used. This led to a two-stage meta-analysis that combined individual participant data with aggregate metadata. RESULTS: We detected four studies (Nâ€?â€?91 women), of which two provided individual participant data (Nâ€?â€?50 women). The composite neonatal outcome occurred in 58/364 (16%) after nifedipine versus 69/359 (19%) after atosiban (OR 0.76, 95%CI 0.47-1.23). Perinatal death occurred in 14/392 (3.6%) after nifedipine versus 7/380 (1.8%) after atosiban (OR 2.0, 95%CI 0.80-5.1). Nifedipine results in longer prolongation of pregnancy, with a 18 days to delivery compared with 10 days for atosiban (HR 0.83 (96% CI 0.69-0.99)). NICU admission occurred less often after nifedipine (46%) than after atosiban (59%), (OR 0.32, 95%CI 0.14-0.75). The sensitivity analysis revealed no difference in prolongation of pregnancy for 48 hours (OR 1.0, 95% CI 0.73-1.4) or 7 days (OR 1.3, 95% CI 0.85-5.8) between nifedipine and atosiban. There was a non-significant higher neonatal mortality in the nifedipine-exposed group (OR 1.4, 95% CI 0.60-3.4). CONCLUSIONS: In this IPDMA, we found no differences in composite outcome between nifedipine and atosiban in the treatment of threatened preterm birth. However, the non-significant higher mortality after administering nifedipine warrants further investigation of the use of nifedipine as a tocolytic drug. STUDY REGISTRATION: We conducted this study according to a prospectively prepared protocol, registered with PROSPERO (the International Prospective Register of Systematic Reviews) under CRD42016024244.

BMC pregnancy and childbirth 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 C9H12O, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Kikuchi, Daisuke published the artcileAntihypertensive drug prescription trends for pregnant women with hypertension in acute hospitals in Japan, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Hypertension Research (2022), 45(9), 1441-1446, database is CAplus and MEDLINE.

Abstract: Hypertensive disorders of pregnancy cause maternal organ damage. Therefore, appropriate management with antihypertensive medication is required from the first trimester. We aimed to clarify the antihypertensive drug prescription trends in pregnant women with hypertension in Japan. The administrative data of pregnant outpatients aged 16-49 years who visited acute hospitals between 2013 and 2020 were included. The annual antihypertensive drug prescription trends were evaluated based on their prescription proportions. The most prescribed drug in 2020 was nifedipine, followed by methyldopa and amlodipine. The proportion of nifedipine prescriptions significantly increased from 33.5 to 40.8% during the study period, whereas that of methyldopa significantly decreased from 16.6 to 11.6%. There was no change in the prescription trend of amlodipine. Dihydropyridine calcium channel blockers were the most commonly prescribed drug for pregnant women with hypertension.

Hypertension Research 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

Nogawa, Hisashi published the artcilePharmacological characterisation of electrocardiogram J-T_peak interval in conscious Guinea pigs, Product Details of C17H18N2O6, the publication is European Journal of Pharmacology (2022), 175065, database is CAplus and MEDLINE.

Drug-induced human ether-a-́go-go-related gene (hERG) channel block and QT interval prolongation increase torsade de pointes (TdP) risk. However, some drugs block hERG channels and prolong QT interval with low TdP risk, likely because they block addnl. inward currents. We investigated the utility of J-T_peak interval, a novel biomarker of inward current block and TdP risk, in conscious telemetered guinea pigs. ECG parameters were analyzed in Hartley guinea pigs orally administered one of eight test compounds (dofetilide, flecainide, nifedipine, quinidine, quinine, ranolazine, sotalol, verapamil) or vehicle alone as controls. Heart rate-corrected QT (QTcX) and J-T_peak (J-T_peakcX) were calculated to evaluate the relations of QT-RR and J-T_peak-RR. Dofetilide and sotalol significantly increased ΔQTcX and ΔJ-T_peakcX intervals to similar degrees. Quinidine, quinine and flecainide also increased ΔQTcX and ΔJ-T_peakcX intervals, but the degrees of ΔJ-T_peakcX interval prolongation were shorter than those of ΔQTcX interval prolongation. Ranolazine showed slight increasing trends in ΔQTcX and ΔJ-T_peakcX intervals, but the differences were not significant. Verapamil and nifedipine did not increase the ΔQTcX or ΔJ-T_peakcX intervals. Based on the relations of ΔΔJ-T_peakcX and ΔΔQTcX intervals, dofetilide, sotalol and quinidine were classified as high risk for TdP, quinine, flecainide and ranolazine were classified as intermediate risk and verapamil and nifedipine were classified as low risk. These results supported the usefulness of J-T_peak interval assessment in conscious guinea pigs for predicting drug-induced balanced block of inward currents and TdP risk in early-stage preclin. studies.

European Journal of 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, Product Details of C17H18N2O6.

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

Kucharski, Dawid published the artcileThe assessment of environmental risk related to the occurrence of pharmaceuticals in bottom sediments of the Odra River estuary (SW Baltic Sea), Quality Control of 21829-25-4, the publication is Science of the Total Environment (2022), 154446, database is CAplus and MEDLINE.

The occurrence of 130 pharmaceutically active compounds (PhACs) in sediments collected from 70 sampling sites in the Odra River estuary (SW Baltic Sea) was investigated. The highest concentration levels of the compounds were found in the vicinity of effluent discharge from two main Szczecin wastewater treatment plants: “Pomorzany” and “Zdroje”, and nearby the seaport and shipyard. The highest environmental risks (RQ > 1) were observed for pseudoephedrine (RQ = 14.0), clindamycin (RQ = 7.3), nalidixic acid (RQ = 3.8), carbamazepine (RQ = 1.8), fexofenadine (RQ = 1.4), propranolol (RQ = 1.1), and thiabendazole (RQ = 1.1). RQ for each compound varied depending on the sampling sites. High environmental risk was observed in 30 sampling sites for clindamycin, 22 sampling sites for pseudoephedrine, 19 sampling sites for nalidixic acid, 4 sampling sites for carbamazepine, and 3 sampling sites for fexofenadine. The medium environmental risk (0.1 < RQ < 1) was observed for 16 compounds: amisulpride, amitriptyline, amlodipine, atropine, bisoprolol, chlorpromazine, lincomycin, metoprolol, mirtazapine, moclobemide, ofloxacin, oxazepam, tiapride, tolperisone, verapamil, and xylometazoline. Due to the scarcity of toxicol. data related to benthic organisms, only an approx. assessment of the environmental risk of PhACs is possible. Nevertheless, the compounds with medium and high risk should be considered as pollutants of high environmental concern whose occurrence in the environment should remain under close scrutiny.

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

Karunanithi, Srividhya published the artcileTocilizumab and Renal Artery Stent-Therapeutic Strategy for Takayasu Arteritis, Synthetic Route of 21829-25-4, the publication is Journal of Clinical Rheumatology and Immunology (2022), 22(1), 37-40, database is CAplus.

Takayasu vasculitis (TAK) is a form of large vessel vasculitis clin. manifesting as pulseless disease or hypertension. It is more common in South East Asia and Japan, India, and Mexico [1]. It is increasingly being recognized due to increased awareness among medical fraternity and better imaging modalities. Undetected hypertension, pulselessness, and syncope are more common symptoms and presentation during pregnancy is unusual and can lead to bad obstetric outcomes. Recent evidences support the use of tocilizumab for inducing remission in Takayasu arteritis. We report this rare case of vasculitis presenting in pregnancy as malignant hypertension. A 20-yr-old pregnant woman (45 days) presented with headache and nausea but no fever. She had a history of intermittent claudication of legs for the past 3 years but not evaluated. During examination, pulses were felt normally and blood pressure (BP) 180/110, no murmurs in cardiac auscultation, but she had abdominal bruit (renal vessels). Other systems were normal. Echocardiogram (ECHO) showed dilated ascending aorta. Doppler of renal vessels showed narrowing of renal arteries. Unfortunately, she had to undergo termination of pregnancy (high BP in spite of antihypertensives). Her computed tomog. (CT) angiogram showed features of TAK with type 5 pattern-she had methylprednisolone infusion 500 mg daily for 3 days, followed by injection tocilizumab 400 mg monthly 3 doses. Once remission was achieved, she had recanalization by percutaneous transluminal angioplasty of right renal artery. She is currently maintained on aspirin and telmisartan. Awareness of causes of high BP, inputs by radiologist, cardiologist, and rheumatologist and understanding by the patient and family helped to achieve good outcome albeit the miscarriage.

Journal of Clinical Rheumatology and Immunology 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

Hate, Siddhi S. published the artcileA Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) (2022), 111(1), 102-115, database is CAplus and MEDLINE.

There is an increasing shift from dissolution testing to dissolution-permeation testing of formulations during formulation development and this has led increasing application of permeability measurements using parallel artificial membrane permeability assay (PAMPA) membranes. However, there is a lack of thorough anal. of the impact of variabilities in the PAMPA setup on the mass flow rate outcomes, particularly for complex solubility-enabling formulations. In this study, we investigated the impact of amorphous drug-rich nanodroplets, formed in supersaturated solutions by liquid-liquid phase separation, on membrane transport by measuring mass flow rate across PAMPA membranes. In addition, we explored the impact of PAMPA variants such as lipid composition, hydrophobicity and pore size of the filter support, as well as receiver sink properties on membrane mass flow rates of solutions containing amorphous nanodroplets. Filter properties and lipid composition did not show a notable influence on the mass flow rates for lipophilic mols., while a marked impact was observed for hydrophilic mols. High sink conditions in the receiver compartment, arising from addition of micellar surfactant, altered the membrane integrity for lipid-impregnated hydrophilic membranes. In contrast, no such effect was observed for a hydrophobic filter support. Membrane integrity tests also suggested that monitoring water transport may be an improved approach over using Lucifer yellow. Furthermore, high sink conditions in the receiver compartment resulted in an increase in the overall mass flow rate. This was due to the effect of asym. conditions, generated across the membrane, on mass transport kinetics. Linearity between mass flow rate and donor concentration was observed until the donor concentration reached the amorphous solubility Above the amorphous solubility, a gradual increase in mass flow rate was observed i.e., with an increasing number of nanodroplets in the solution This was attributed to decrease in the permeability barrier across unstirred water layer due to reduction of the concentration gradient as nanodroplets dissolved to replenish absorbed drug. Observations made in this study provide insights into the mechanisms associated with mass transport of supersaturated solutions across PAMPA membranes, which are critical for improved evaluation of enabling formulations.

Journal of Pharmaceutical Sciences (Philadelphia, PA, 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, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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