Category: pyridine-derivatives

Chatzistavraki, Maria published the artcileAmyloid β-protein precursor regulates depolarization-induced calcium-mediated synaptic signaling in brain slices, SDS of cas: 21829-25-4, the main research area is amyloid protein depolarization calcium signaling brain slice; Alzheimer’s disease; AβPP; amyloid-β protein precursor; calcium; neuronal signaling; synapse.

Coordinated calcium influx upon neuronal depolarization activates pathways that phosphorylate CaMKII, ERKs, and the transcription factor CREB and, therefore, expression of pro-survival and neuroprotective genes. Recent evidence indicates that amyloid-β protein precursor (AβPP) is trafficked to synapses and promotes their formation. At the synapse, AβPP interacts with synaptic proteins involved in vesicle exocytosis and affects calcium channel function. Herein, we examined the role of AβPP in depolarization-induced calcium-mediated signaling using acute cerebral slices from wild-type C57bl/6 mice and AβPP-/- C57bl/6 mice. Depolarization of acute cerebral slices from wild-type C57bl/6 and AβPP-/- C57bl/6 mice was used to induce synaptic signaling. Protein levels were examined by western blot and calcium dynamics were assessed using primary neuronal cultures. In the absence of AβPP, decreased pCaMKII and pERKs levels were observed This decrease was sensitive to the inhibition of N- and P/Q-type Voltage Gated Calcium Channels (N- and P/Q-VGCCs) by ω-conotoxin GVIA and ω-conotoxin MVIIC, resp., but not to inhibition of L-type VGCCs by nifedipine. However, the absence of AβPP did not result in a statistically significant decrease of pCREB, which is a known substrate of pERKs. Finally, using calcium imaging, we found that down regulation of AβPP in cortical neurons results in a decreased response to depolarization and altered kinetics of calcium response. AβPP regulates synaptic activity-mediated neuronal signaling by affecting N- and P/Q-VGCCs.

Journal of Alzheimer’s Disease 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, SDS of cas: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wadsworth, Harry published the artcileExploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein-potential novel positron emitting tomography imaging agents, Formula: C7H7NO2, the main research area is PET imaging diaryl anilide preparation translocator protein ligand SAR.

A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesized and evaluated as potential positron emitting tomog. (PET) ligands for imaging TPSO in vivo. Fluorine-18 labeling of the mols. was achieved using direct radiolabelling or synthon based labeling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clin. imaging agents.

Bioorganic & Medicinal Chemistry Letters published new progress about Brain. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Asakawa, Chiharu published the artcile[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice, Application of Methyl 4-chloropicolinate, the main research area is carbon 11 sorafenib preparation PET imaging brain.

Sorafenib (Nexavar, BAY43-9006, 1) is a second-generation, orally active multikinase inhibitor that is approved for the treatment of some cancers in patients. In this Letter, we developed [11C]1 as a novel positron emission tomog. (PET) probe, and evaluated the influence of ABC transporters-mediated efflux on brain uptake using PET with [11C]1 in P-glycoprotein (P-gp)/breast cancer resistance protein (Bcrp) knockout mice vs. wild-type mice. [11C]1 was synthesized by the reaction of hydrochloride of aniline 2 with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]6, followed by reaction with another aniline 3. Small-animal PET study with [11C]1 indicated that the radioactivity level (AUC0-60 min, SUV × min) in the brains of P-gp/Bcrp knockout mice was about three times higher than in wild-type mice.

Bioorganic & Medicinal Chemistry Letters published new progress about Brain. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Application of Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jamei, Masoud published the artcileCurrent status and future opportunities for incorporation of dissolution data in PBPK modeling for pharmaceutical development and regulatory applications: OrBiTo consortium commentary, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is pharmaceutical pharmacokinetics felodipine ibuprofen; Biorelevant dissolution; Dissolution; Oral drug absorption; PBBM (Physiologically Based Biopharmaceutical Model); PBPK.

In vitro dissolution experiments are used to qual. assess the impact of formulation composition and process changes on the drug dosage form performance. However, the use of dissolution data to quant. predict changes in the absorption profile remains limited. Physiol.-based Pharmacokinetic(s) (PBPK) models facilitate incorporation of in vitro dissolution experiments into mechanistic oral absorption models to predict in vivo oral formulation performance, and verify if the drug product dissolution method is biopredictive or clin. relevant. Nevertheless, a standardized approach for using dissolution data within PBPK models does not yet exist and the introduction of dissolution data in PBPK relies on a case by case approach which accommodates from differences in release mechanism and limitations to drug absorption. As part of the Innovative Medicines Initiative (IMI) Oral Biopharmaceutics Tools (OrBiTo) project a cross-work package was set up to gather a realistic understanding of various approaches used and their areas of applications. This paper presents the approaches shared by academic and industrial scientists through the OrBiTo project to integrate dissolution data within PBPK software to improve the prediction accuracy of oral formulations in vivo. Some general recommendations regarding current use and future improvements are also provided.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Cecum. 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

Locatelli, Marcello published the artcileFabric-Phase Sorptive Membrane Array As a Noninvasive In Vivo Sampling Device For Human Exposure To Different Compounds, Category: pyridine-derivatives, the main research area is fabric sorption membrane array human exposure sampling device.

This study introduces an innovative device for the noninvasive sampling and chromatog. anal. of different compounds present in exhaled breath aerosol (EBA). The new sampling device, especially in light of the recent COVID-19 pandemic that forced many countries to impose mandatory facemasks, allows an easy monitoring of the subject′s exposure to different compounds they may come in contact with, actively or passively. The project combines the advantages of a fabric-phase sorptive membrane (FPSM) as an in vivo sampling device with a validated LC-MS/MS screening procedure able to monitor more than 739 chems. with an overall anal. time of 18 min. The project involves the noninvasive in vivo sampling of the EBA using an FPSM array inserted inside an FFP2 mask. The study involved 15 healthy volunteers, and no restrictions were imposed during or prior to the sampling process regarding the consumption of drinks, food, or drugs. The FPSM array-LC-MS/MS approach allowed us to effectively exploit the advantages of the two complementary procedures (the convenient sampling by an FPSM array and the rapid anal. by LC-MS/MS), obtaining a powerful and green tool to carry out rapid screening analyses for human exposure to different compounds The flexible fabric substrate, the sponge-like porous architecture of the high-efficiency sol-gel sorbent coating, the availability of a large cache of sorbent coatings, including polar, nonpolar, mixed mode, and zwitterionic phases, the easy installation into the facemask, and the possibility of sampling without interrupting regular activities provide FPSMs unparalleled advantages over other sampling techniques, and their applications are expected to expand to many other clin. or toxicol. studies.

Analytical Chemistry (Washington, DC, United States) published new progress about Drugs. 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

Zhao, Lixiang published the artcileElectrospun fixed dose combination fibers for the treatment of cardiovascular disease, Category: pyridine-derivatives, the main research area is electrospun fibers cardiovascular disease; Amorphous solid dispersion; Electrospinning; Fixed dose combination; Nanofiber; Nifedipine; Spironolactone.

Fixed dose combinations (FDCs) offer an accessible way to simplify complex therapeutic regimens by the simultaneous presentation of multiple drugs in a single entity to the patient. However, encapsulation of hydrophobic drugs into FDCs possess a number of tech. challenges. Electrospinning comprises a convenient way to incorporate multiple hydrophobic drugs into a single formulation in a single step, via the use of an appropriate organic solvent system during fabrication. In this study, we report a series of novel fiber formulations comprising Et cellulose loaded with two hydrophobic drugs, spironolactone and nifedipine, either individually or in combination. The drugs are found to be present in the fibers in the form of amorphous solid dispersions, and these are stable at room temperature for 4 mo. The products showed extended release profiles over more than 30 h. This formulation strategy offers potential to manage chronic cardiovascular conditions and overcome patient related non-adherence by providing a simplified treatment model.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Drugs. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhao, Junli published the artcileBerberine mediated positive inotropic effects on rat hearts via a Ca2+-dependent mechanism, Category: pyridine-derivatives, the main research area is berberine inotropic agent heart calcium; Ca2+; Na+; berberine; heart; positive inotropic effect.

Previous studies showed that berberine, an alkaloid from Coptis Chinensis Franch, might exert a pos. inotropic effect on the heart. However, the underlying mechanisms were unclear. Here, we reported that berberine at 10-20μM increased the left ventricular (LV) developed pressure and the maximal rate of the pressure rising, and it increased the maximal rate of the pressure descending at 20μM in Langendorff-perfused isolated rat hearts. These effects diminished with the concentration of berberine increasing to 50μM. In the concentration range of 50-300μM, berberine increased the isometric tension of isolated left ventricular muscle (LVM) strips with or without elec. stimulations, and it (30-300μM) also increased the intracellular Ca2+ level in the isolated LV myocytes. The removal of extracellular Ca2+ hindered the berberine-induced increases in the tension of LVM strips and the intracellular Ca2+ level of LV myocytes. These suggested that berberine might exert its pos. inotropic effects via enhancing Ca2+ influx. The blockade of L-type Ca2+ channels (LTCCs) with nifedipine significantly attenuated 300 mM berberine-induced tension increase in LVM strips but not the increase in the intracellular Ca2+ level. Berberine (300 mM) further increased the LVM tension following the treatment with the LTCC opener FPL-64716 (10 mM), indicating an LTCC-independent effect of berberine. Lowering extracellular Na+ attenuated the berberine-induced increases in both the tension of LVM strips and the intracellular Ca2+ level of LV myocytes. In conclusion, berberine might exert a pos. inotropic effect on the isolated rat heart by enhancing the Ca2+ influx in LV myocytes; these were extracellular Na+ -dependent.

Frontiers in Pharmacology published new progress about Heart. 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, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Moreau, Magali published the artcileA baseline assessment of emerging organic contaminants in New Zealand groundwater, Product Details of C18H19Cl2NO4, the main research area is emerging organic contaminant baseline assessment groundwater pollution New Zealand; Emerging organic contaminant; Groundwater; Groundwater quality; Monitoring; New Zealand; Waikato region.

Emerging organic contaminants (EOC) are manufactured compounds, used for a variety of purposes, are a rising concern for freshwater quality and human and aquatic health. Their occurrence in groundwater was demonstrated in several international surveys. This work conducted the first baseline survey on EOC occurrence in New Zealand groundwater, using a wide-screening approach (723 compounds) and a novel stratified to mean residence time (MRT) randomized design to inform future monitoring. A total of 61 sites were sampled: 51 baseline sites from State of the Environment network in the Waikato region, and 10 targeted sites near known EOC sources for comparison. EOC were detected at 91% of baseline sites at concentrations of 0.1-11,000 ng/L. Multiple EOC groups were encountered: pesticides (48 compounds), pharmaceuticals (11), industrial (10), preservatives/food additives (3), and personal care products (1). Similar EOC diversity and concentration range were observed at targeted sites, with the addition of drugs of abuse and life-style compounds EOC detections occurred across young (1-11 yr. MRT), intermediate (11-50 yr. MRT), and old (50-250 yr. MRT) groundwater with higher concentrations and more types of EOC detected at sites with the youngest groundwater. Concentrations of 73 compounds detected at baseline sites were comparable to those observed in overseas groundwater, with 28 compounds measured at concentrations greater than the European Union maximum admissible concentration for pesticides. Survey results were used to: review current pesticide monitoring; propose complementary monitoring; identify potential EOC groundwater tracers; and identify compounds for which cost-effective, national laboratory capability is needed. Waikato survey results demonstrated ubiquitous occurrence of un-monitored, unregulated EOC in groundwater and limitations for using targeted approaches to establish monitoring.

Science of the Total Environment published new progress about Aquifers. 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

Mohammed, Atyaf Hasan published the artcileA comparative study among effects of treatment with nifedipine, verapamil, diazepam or alpha-methyldopa on platelets count and behavior in women with preeclampsia, COA of Formula: C17H18N2O6, the main research area is preeclampsia nifedipine verapamil diazepam alpha methyldopa platelet behavior.

This study was conducted to investigate the role of platelets -count and -be- havior in the pathogenesis of mild and moderate preeclampsia (PE). Also, the effects of the specific treatment regimen in both cases of preeclampsia inves- tigated. In mild PE only nifedipine had significantly higher platelet count compared to those without treatment, while in moderate PE both verapamil and nifedipine had significantly higher platelet count compared to those without treatment. Concerning platelet response to ADP; in mild PE all drugs show an increase in response compared to those without treatment, a similar finding reported in moderate. While platelet response to collagen, in mild PE both diazepam and verapamil show increased response compared to those without treatment, in moderate PE methyldopa and verapamil show in- creased response compared to those without treatment. In conclusion, plate- lets may be involved in the pathogenesis of preeclampsia. Nifedipine and ve- rapamil produced effective enhancement of ex vivo platelets aggregation-in- duced by ADP or collagen and may evolve as antiplatelet agents that able to prevent the in vivo activation of platelets and exhaustion cycle, an action which could explain the observed effectiveness of calcium channel blockers for the prevention and treatment of preeclampsia other than diazepam or al- pha-methyldopa used in this study.

International Journal of Research in Pharmaceutical Sciences (Madurai, India) published new progress about Behavior. 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, COA of Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

van Winden, Tms published the artcileEffects of tocolysis with nifedipine or atosiban on child outcome: follow-up of the APOSTEL III trial, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is nifedipine atosiban preterm birth; Atosiban; behaviour; child; development; executive function; follow-up; health; infant; neurodevelopment; nifedipine; preterm birth; preterm labour; tocolysis.

Objective : To compare the long-term effects of tocolysis with nifedipine or atosiban on child outcome at age 2.5-5.5 years. Design : The APOSTEL III trial was a multicentre randomised controlled trial that compared tocolysis with nifedipine or atosiban in 503 women with threatened preterm birth. Methods : Parents were asked to complete four questionnaires regarding neurodevelopment, executive function, behavior problems and general health. Main outcome measures : The main long-term outcome measure was a composite of abnormal development at the age of 2.5-5.5 years. Results : Of the 426 women eligible for follow-up, 196 parents returned the questionnaires for 115 children in the nifedipine group and 110 children in the atosiban group. Abnormal development occurred in 32 children in the nifedipine group and in 38 children in the atosiban group (OR 0.74, 95% CI 0.41-1.34). Sensitivity anal. for all children of the APOSTEL III trial, including a comparison of deceased children, resulted in a higher rate of healthy survival in the nifedipine group (64 vs. 54%), but there was no significant difference in the overall mortality rate (5.4 vs. 2.7%). Conclusion : Outcomes on broad child neurodevelopment, executive function, behavior and general health were comparable in both groups. Tweetable abstract : Nifedipine- and atosiban-exposed children had comparable long-term outcomes, including neurodevelopment, executive function and behavior.

BJOG published new progress about Behavior. 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