Category: pyridine-derivatives

Ding, Shengang published the artcileInflammatory cytokines tumour necrosis factor-α and interleukin-8 enhance airway smooth muscle contraction by increasing L-type Ca2+ channel expression, Quality Control of 21829-25-4, the main research area is TNFalpha IL8 airway smooth muscle contraction LVDCC asthma; IL-8; L-type Ca2+ channel; TNF-α; airway smooth muscle; asthma; inflammation.

Inflammation elevates intracellular calcium concentrations ([Ca2+]i) in airway smooth muscle (ASM). The L-type Ca2+ channel (L-VDCC) plays an important role in regulating Ca2+ influx in ASM. However, the role of L-VDCC in the inflammatory cytokine-induced pathol. of ASM remains unclear. In the present study, we used calcium imaging and isometric tension measurements to assess the role of L-VDCC in agonist-induced [Ca2+]i rise and the associated contractions in mouse ASM, and we used immunoblotting to identify L-VDCC protein expression levels in mouse ASM after exposure to tumor necrosis factor alpha (TNF-a) or interleukin-8 (IL-8). Our results showed that high-K+- or carbachol-induced contractions of mouse ASM were significantly greater after pretreatment with TNF-α or IL-8 for 24 h. Both verapamil and nifedipine, L-VDCC inhibitors, abolished this increased contraction induced by TNF-α or IL-8 pretreatment. Moreover, TNF-α treatment enhanced carbachol-induced Ca2+ influx in ASM cells, and this effect was abrogated by verapamil. Addnl., immunoblotting results showed that preincubation of mouse ASM with TNF-α or IL-8 also enhanced L-VDCC protein expression. On the basis of these findings, we concluded that proinflammatory cytokines, such as TNF-α and IL-8, increase the expression level of L-VDCC, which in turn contributes to augmented agonist-induced ASM contractions. This effect of inflammation on L-VDCC expression in ASM may be associated with airway hyper-responsiveness and involved in the development of asthma.

Clinical and Experimental Pharmacology and Physiology published new progress about Asthma. 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, Quality Control of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tingle, Samuel J. published the artcileCalcium channel blockers in pancreatic cancer: increased overall survival in a retrospective cohort study, Related Products of pyridine-derivatives, the main research area is pancreatic cancer hypertension Iercanidipine amlodipine calcium channel blocker.

This retrospective cohort study aimed to translate this into the clinic by investigating the effect of CCBs on survival in pancreatic cancer. One hundred sixty-four patients with unresectable pancreatic ductal adenocarcinoma were included. Data were collected on CCB prescription, and for a range of other potentially important prognostic factors: ECOG performance status, AJCC cancer stage, chemotherapy regimen, radiotherapy, age, hypertension and sex. Participants prescribed CCB (n = 30) were more likely to be older (P = 0.004) and have hypertension (P < 0.0005); baseline demographics were otherwise similar between groups. On adjusted cox regression patients prescribed CCBs demonstrated significantly improved overall survival; hazard ratio -0.496 (0.297-0.827; P = 0.007). Performance status (P < 0.0005), tumor stage (P < 0.0005), chemotherapy regimen (P < 0.0005), radiotherapy (0.002) and age (P = 0.012) were also independent predictors of survival. The Kaplan-Meier estimated median survival was 15.3 mo for patients prescribed CCBs vs. 10.1 mo for patients not prescribed CCBs (P = 0.131). This study supports previous work suggesting CCBs may be beneficial in pancreatic cancer. Further work on larger datasets will allow for subgroup anal. delineating the effects of specific CCBs in combination with different forms of chemotherapy, paving the way for future prospective studies. Anti-Cancer Drugs published new progress about Biopsy. 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tingle, Samuel J. published the artcileCalcium channel blockers in pancreatic cancer: increased overall survival in a retrospective cohort study, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pancreatic cancer hypertension Iercanidipine amlodipine calcium channel blocker.

This retrospective cohort study aimed to translate this into the clinic by investigating the effect of CCBs on survival in pancreatic cancer. One hundred sixty-four patients with unresectable pancreatic ductal adenocarcinoma were included. Data were collected on CCB prescription, and for a range of other potentially important prognostic factors: ECOG performance status, AJCC cancer stage, chemotherapy regimen, radiotherapy, age, hypertension and sex. Participants prescribed CCB (n = 30) were more likely to be older (P = 0.004) and have hypertension (P < 0.0005); baseline demographics were otherwise similar between groups. On adjusted cox regression patients prescribed CCBs demonstrated significantly improved overall survival; hazard ratio -0.496 (0.297-0.827; P = 0.007). Performance status (P < 0.0005), tumor stage (P < 0.0005), chemotherapy regimen (P < 0.0005), radiotherapy (0.002) and age (P = 0.012) were also independent predictors of survival. The Kaplan-Meier estimated median survival was 15.3 mo for patients prescribed CCBs vs. 10.1 mo for patients not prescribed CCBs (P = 0.131). This study supports previous work suggesting CCBs may be beneficial in pancreatic cancer. Further work on larger datasets will allow for subgroup anal. delineating the effects of specific CCBs in combination with different forms of chemotherapy, paving the way for future prospective studies. Anti-Cancer Drugs published new progress about Biopsy. 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

Micucci, Matteo published the artcileCastanea sativa Mill. bark extract cardiovascular effects in a rat model of high-fat diet, HPLC of Formula: 21829-25-4, the main research area is Castanea sativa cardiovascular effect high fat diet Ellagitannin; cholinergic receptor; chronotropy; hydrolysable tannins; inotropy; oxydative stress; vascular relaxation.

Ellagitannins may have a beneficial impact in cardiovascular diseases. The aim of the study was to evaluate the effect of high-fat diet (HFD) and the efficacy of Castanea sativa Mill. bark extract (ENC) on cardiac and vascular parameters. Rats were fed with regular diet, (RD, n = 15), HFD (n = 15), RD + ENC (20 mg/kg/day by gavage, n = 15), and HFD + ENC (same dose, n = 15) and the effects on body weight, biochem. serum parameters, and inflammatory cytokines determined Cardiac functional parameters and aorta contractility were also assessed on isolated atria and aorta. Results showed that ENC reduced weight gain and serum lipids induced by HFD. In in vitro assays, HFD decreased the contraction force of left atrium, increased right atrium chronotropy, and decreased aorta K+-induced contraction; ENC induced transient pos. inotropic and neg. chronotropic effects on isolated atria from RD and HFD rats and a spasmolytic effect on aorta. In ex vivo experiments, ENC reverted inotropic and chronotropic changes induced by HFD and enhanced Nifedipine effect more on aorta than on heart. In conclusion, ENC restores metabolic dysfunction and cardiac cholinergic muscarinic receptor function, and exerts spasmolytic effect on aorta in HFD rats, highlighting its potential as nutraceutical tool in obesity.

Phytotherapy Research published new progress about Aorta. 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Tepech-Carrillo, Carlos published the artcileStudy of the reactivity of (100) felodipine surface model based on DFT concepts, Formula: C18H19Cl2NO4, the main research area is felodipine reactivity density functional theory surface model.

In this study, D. Functional Theory including a dispersion correction is employed to model and analyze the structural, electronic and local reactivity of the (100) surface of felodipine. The surface energy calculated at the Generalized Gradient Approximation (GGA) level, along with plane waves as basis set and ultrasoft pseudopotentials, shows that the (100) surface is the most stable as compared to the (010) and (110) ones. In particular, we have focused on performing a quant. study of the reactivity of the surface by means of the Fukui function and through the HOMO and LUMO populations. Our results can be related to some applications in the pharmaceutical chem. of this compound

Open Journal of Physical Chemistry published new progress about Atoms. 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, Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Han, Xiuyuan published the artcileEffect Of epigallocatechin-3-gallate on the pharmacokinetics of amlodipine in rats, Product Details of C18H19Cl2NO4, the main research area is liver microsome amlodipine EGCG pharmacokinetics; Drug–drug interaction; EGCG; LC-MS/MS; amlodipine; pharmacokinetics.

This study investigates the effect of epigallocatechin-3-gallate (EGCG), a major ingredient of green tea, on the pharmacokinetics of amlodipine in rats. The pharmacokinetics of orally administered amlodipine (1 mg/kg) with or without EGCG pretreatment (30 mg/kg/day for 10 days) were investigated. Plasma concentrations of amlodipine were determined by using a sensitive and reliable liquid chromatog. with tandem mass spectroscopy (LC-MS/MS) method. The effects of EGCG on the metabolic stability of amlodipine were investigated by using rat liver microsome incubation systems. The results indicated that when the rats were pretreated with EGCG, the Cmax of amlodipine increased from 16.32 ± 2.57 to 21.44 ± 3.56 ng/mL (p < 0.05), the Tmax decreased from 5.98 ± 1.25 to 4.01 ± 1.02 h (p < 0.05), and the AUC0-t increased from 258.12 ± 76.25 to 383.34 ± 86.95 mug h L-1 (p < 0.05), which suggested that the pharmacokinetic behavior of amlodipine was affected after oral co-administration of EGCG. Addnl., the metabolic half-life was prolonged from 31.3 ± 5.6 to 52.6 ± 7.9 min (p < 0.05) with the pretreatment of EGCG. It can be speculated that the drug-drug interaction between EGCG and amlodipine might occur, which might have resulted from the metabolism inhibition of amlodipine by EGCG when they were co-administered. Xenobiotica published new progress about Blood. 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, Product Details of C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Adeyemi, Oladipupo published the artcileA pharmacological characterization of electrocardiogram PR and QRS intervals in conscious telemetered rats, Application In Synthesis of 21829-25-4, the main research area is ECG pharmacol agent radiotelemetry; Diltiazem; Electrocardiogram; Flecainide; Methods; Nifedipine; Quinidine; Rat; Telemetry; Translation; Verapamil.

The current study aimed to identify its utility in assessing ECG (ECG) PR and QRS interval changes. Male Han-Wistar rats (~250 g) were implanted with radio-telemetry devices for the recording of ECG and haemodynamic parameters. Animals (n = 4-8) were treated with single doses of calcium (nifedipine, diltiazem or verapamil; CCBs) or sodium channel blockers (quinidine or flecainide; SCBs) or their corresponding vehicles in an ascending dose design. Pharmacokinetic anal. of blood samples was performed to allow comparison of effects to published data in other species. Of the CCBs, only diltiazem (300 mg/kg) prolonged the PR interval (49 ± 2 vs. vehicle: 43 ± 1 ms), although this was not statistically significant (p = .11). QA interval decreased with nifedipine (30 ± 1 vs. 24 ± 0 ms) and diltiazem (34 ± 1 vs. 27 ± 1 ms) but increased with verapamil (30 ± 0 vs. 37 ± 1 ms) demonstrating pharmacol. activity of each agent. Both SCBs, caused statistically significant (p < .05) increases in both intervals - quinidine (100 mg/kg; PR: 50 ± 2 vs. 43 ± 1 ms; QRS: 22 ± 2 vs. 18 ± 1 ms) and flecainide (9 mg/kg; PR: 56 ± 1 vs. 46 ± 1 ms; QRS: 27 ± 1 vs. 21 ± 1 ms). At similar plasma concentrations to other species, the conscious telemetered rat demonstrates limited utility in assessing PR interval prolongation by CCBs, despite significant contractility effects being observed However, results with SCBs demonstrate a potential application for evaluating drug-induced QRS prolongation. Journal of Pharmacological and Toxicological Methods published new progress about Blood. 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

Kim, Hyung Min published the artcileSimultaneous determination of cardiovascular drugs in dried blood spot by liquid chromatography-tandem mass spectrometry, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is blood cardiovascular drug amlodipine atenolol atorvastatin digoxin LC MS; Cardiovascular drugs; Dried blood spot; LC-MS/MS; Therapeutic drug monitoring.

A dried blood spot (DBS) sampling method was exploited to extract cardiovascular drugs using a small volume of whole blood of human and rodent. Thereafter, an anal. method using liquid chromatog. with tandem mass spectrometry (LC-MS/MS) was developed and validated for the determination of 12 cardiovascular drugs. A 6 mm internal diameter disk containing 10μL of blood was punched from a specifically designed card and analyzed by LC-MS/MS using a gradient elution method with a total run time of 16 min. For sample separation, a universal octadecyl-silica column was used with a flow rate of 0.2 mL/min. The developed method was validated in terms of linearity, accuracy, and precision, which showed satisfactory results. In addition, the matrix effects were closely investigated to confirm the extraction efficiency. Addnl., the stability was tested by storing DBSs at room temperature; the results showed that these drugs were stable for at least 30 days. Accordingly, the proposed LC-MS/MS method is capable to analyze several cardiovascular drugs in a single anal. It can be applied to therapeutic drug monitoring in patients as well as in the in vivo settings.

Journal of Food and Drug Analysis published new progress about Blood. 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, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cornelissen, Lisa G. H. published the artcileThe diagnostic value of fetal fibronectin testing in clinical practice, Product Details of C17H18N2O6, the main research area is fetal fibronectin testing diagnostic value; cervical length; cervical length measurement; fetal fibronectin; preterm delivery.

To evaluate the clin. management to withhold treatment for preterm labor in symptomatic women with an intermediate cervical length and neg. fetal fibronectin (fFN) testing. A retrospective cohort study was performed in a tertiary care teaching hospital in the Netherlands. Pregnant women with a gestational age between 23+5 to 34+0 weeks, with the presence of regular uterine contractions accompanied by a cervical length between 15 and 30 mm and intact membranes, who underwent fFN testing were included to obtain the diagnostic value of fFN testing for preterm delivery within 7 days. Fetal fibronectin testing has an extremely high neg. predictive value (100%) and sensitivity (100%) for delivery within 7 days, in singleton and multiple pregnancies. However, specificity (64%) and pos. predictive value (10%) of fFN testing in singleton pregnancies are low. Blood present on the fFN sample does not affect the reliability of the fFN test; the neg. predictive value remains 100%. Women with symptoms of early preterm labor, intact membranes, a cervical length between 15 and 30 mm and neg. fFN testing do not deliver within 7 days. Administration of corticosteroids and tocolytics can safely be withhold. Furthermore, blood on the fFN sample does not change the reliability of the fFN test.

Journal of Obstetrics and Gynaecology Research published new progress about Blood. 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

Rousset, Matthieu published the artcileMammalian Brain Ca2+ Channel Activity Transplanted into Xenopus laevis Oocytes, Quality Control of 21829-25-4, the main research area is calcium channel Xenopus laevis oocyte mammalian brain; CaV2 Ca2+ channels; channelopathies; membrane microtransplantation; voltage clamp.

Several mutations on neuronal voltage-gated Ca2+ channels (VGCC) have been shown to cause neurol. disorders and contribute to the initiation of epileptic seizures, migraines, or cerebellar degeneration. Anal. of the functional consequences of these mutations mainly uses heterologously expressed mutated channels or transgenic mice which mimic these pathologies, since direct electrophysiol. approaches on brain samples are not easily feasible. We demonstrate that mammalian voltage-gated Ca2+ channels from membrane preparation can be microtransplanted into Xenopus oocytes and can conserve their activity. This method, originally described to study the alteration of GABA receptors in human brain samples, allows the recording of the activity of membrane receptors and channels with their native post-translational processing, membrane environment, and regulatory subunits. The use of hippocampal, cerebellar, or cardiac membrane preparation displayed different efficacy for transplanted Ca2+ channel activity. This technique, now extended to the recording of Ca2+ channel activity, may therefore be useful in order to analyze the calcium signature of membrane preparations from unfixed human brain samples or normal and transgenic mice.

Membranes (Basel, Switzerland) published new progress about Brain. 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, Quality Control of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem