Category: pyridine-derivatives

Yao, Jun published the artcileNifedipine inhibits oxidative stress and ameliorates osteoarthritis by activating the nuclear factor erythroid-2-related factor 2 pathway, Synthetic Route of 21829-25-4, the main research area is osteoarthritis nifedipine oxidative stress Nrf2; Inflammation; Nifedipine; Nrf2/HO-1 pathway; Osteoarthritis; Oxidative stress.

Nifedipine is a voltage-gated calcium channel inhibitor widely used in the treatment of hypertension. Nifedipine has been reported to have antioxidant and anti-apoptotic effects and promotes cell proliferation. However, the effects of nifedipine on oxidative stress and apoptosis in osteoarthritic (OA) chondrocytes are still unclear. In this study, we sought to investigate whether nifedipine alleviates oxidative stress and apoptosis in OA through nuclear factor erythroid-2-related factor 2 (Nrf2) activation. The cytotoxicity of nifedipine against human chondrocytes was detected using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) kit, whereas mRNA and protein expression levels were measured using reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting, resp. The oxidative stress level was analyzed by measuring reactive oxygen species (ROS), glutathione peroxidase (GSH-px), catalase (CAT) and superoxide dismutase (SOD) activities. The role of Nrf2 in the effect of nifedipine on OA was analyzed using an Nrf2 inhibitor brusatol (BR). The result showed that nifedipine inhibited the expression of matrix metalloprotein(MMP)-13, interleukin (IL)-1β, IL-6, tumor necrosis factor (TNF)-α, cyclooxygenase (COX)-2, inducible nitric oxide (NO) synthase (iNOS), and prostaglandin E2 (PGE2), as well as reduced ROS production in human OA chondrocytes, which was partially reversed by BR. Nifedipine prevented cartilage degeneration and contributed to the expression of Nrf-2 in chondrocytes. These results indicate that nifedipine inhibited inflammation and oxidative stress in chondrocytes via activation of Nrf-2/HO-1 signaling.

Life Sciences published new progress about Aggrecans Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Synthetic Route of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Asante, Du-Bois published the artcileAnti-inflammatory, anti-nociceptive and antipyretic activity of young and old leaves of Vernonia amygdalina, SDS of cas: 21829-25-4, the main research area is Vernonia leaf anti inflammatory nociceptive antipyretic; Aspirin; Cold allodynia; Diclofenac; Edema; Mast cells; Paw withdrawal; Pyrexia; Vernonia amygdalina.

Both young and old leaves of Vernonia amygdalina (VA) are traditionally used to treat inflammation, pain and fever. However, the efficacy of young and old leaves for treating these ailments have not been compared till date. To ascertain the effect of young and old leaves of VA in managing inflammation, pain and fever. Both quant. and qual. phytochem. screening of ethanol extracts of young (EthYL) and old (EthOL) leaves of VA were performed. The anti-inflammatory activity of orally administered Et and EthOL (50-200 mg/kg) and Diclofenac (10 mg/kg) were evaluated in carrageenan-induced inflammation model in rats. Antipyretic activity of Et, EthOL and Aspirin (25 mg/kg) were assessed in the Baker’s yeast-induced pyrexia model. Anti-allodynic effect of both extracts were evaluated by inserting inflamed paws of rats in cold water. Antinociceptive property of the extracts were assessed using tail withdrawal and formalin-induced nociception test. Histopathol. examination of the paws was performed, in addition to formalin test to understand the possible mechanism of action of the extracts Neg. control rats received 2 mL/kg normal saline in all tests. The amount of flavonoids, alkaloids, tannins, and phenolics were significantly (p < 0.05) higher in EthOL than Et, while saponins were significantly higher (p < 0.05) in Et than EthOL. The antioxidant ability and total antioxidant capacity were significantly (p < 0.05) higher in Et than EthOL. However, this was significantly (p < 0.05) lower than the anti-oxidant activity of Ascorbic acid. A dose-dependent increase in anti-inflammatory, antipyretic and antinociceptive properties were observed in both Et and EthOL, similar to the standard drugs. Mast cell degranulation accompanied by vasodilatation and high leukocytosis were observed in the neg. control, but were markedly low in extract treated groups. Both extracts mediated their analgesic effect through opioidergic and nitric oxide pathways with Et addnl. implicating the muscarinic cholinergic system. Although both Et and EthOL alleviate inflammation, pyrexia and nociception, Et of VA was found to be more potent than EthOL. Biomedicine & Pharmacotherapy published new progress about Alkaloids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Nakayama, Yohei published the artcileFollicular dendritic cell-secreted protein gene expression is upregulated and spread in nifedipine-induced gingival overgrowth, HPLC of Formula: 21829-25-4, the main research area is gingival dendritic cell gene expression; AMTN; FDC-SP; Gingival overgrowth; Junctional epithelium; Nifedipine.

Abstract: Follicular dendritic cell-secreted protein (FDC-SP) is secreted protein expressed in follicular dendritic cells, periodontal ligament and junctional epithelium (JE). Its expression could be controlled during inflammatory process of gingiva; however, responsible mechanism for gingival overgrowth and involvement of FDC-SP in clin. condition is still unclear. We hypothesized that JE-specific genes are associated with the initiation of drug-induced gingival enlargement called gingival overgrowth, and investigated the changes of JE-specific genes expression and their localization in overgrown gingiva from the patients. Immunohistochem. anal. revealed that the FDC-SP localization was spread in overgrown gingival tissues. FDC-SP mRNA levels in GE1 and Ca9-22 cells were increased by time-dependent nifedipine treatments, similar to other JE-specific genes, such as Amelotin (Amtn) and Lamininβ3 subunit (Lamβ3), whereas type 4 collagen (Col4) mRNA were decreased. Immunocytochem. anal. showed that FDC-SP, AMTN, and Lamβ3 protein levels were increased in GE1 and Ca9-22 cells. Transient transfection analyses were performed using luciferase constructs including various lengths of human FDC-SP gene promoter, nifedipine increased luciferase activities of -345 and -948FDC-SP constructs. These results raise the possibility that the nifedipine-induced FDC-SP may be related to the mechanism responsible for gingival overgrowth does not occur at edentulous jaw ridges.

Odontology published new progress about Amelotins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Zimmermann, Viktor published the artcileChemoselective reduction of nitroarenes in the presence of acid-sensitive functional groups: Solid-phase syntheses of amino aryl azides and benzotriazoles, Application In Synthesis of 36437-30-6, the main research area is chemoselective reduction nitroarene acid sensitive functional group present; solid phase synthesis amino aryl azide benzotriazole.

The authors demonstrated the 1st chemoselective reduction of nitroarenes on solid supports in the presence of other reducible functional groups such as triazenes. A unique combination of a single-electron transfer reagent (viologen) with Na2S proved to be convenient in terms of reducing the strength and for the workup. The relatively long reaction times appear justified, considering the possibilities for further diversification of yielded aminoarenes on solid supports. From o-nitroanilines, for example, >95% 5-methyl-1H-benzotriazole was obtained from 5-methyl-2-nitroaniline via formation of the diazonium tetrafluoroborate, reaction with [(benzylamino)methyl]-modified polystyrene (from Merrifield resin) to give a supported triazene, selective reduction using Na2S/K2CO3/1,1′-dioctyl-4,4′-bipyridinium(2+) dibromide, and cleavage of the resin using 5% trifluoroacetic acid in the presence of TMSN3. Azidoanilines were formed by the above sequence from 4-nitroaniline and Me 5-amino-2-nitrobenzoate.

Journal of Combinatorial Chemistry published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation) (azido). 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Application In Synthesis of 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Shutao published the artcileFelodipine enhances aminoglycosides efficacy against implant infections caused by methicillin-resistant Staphylococcus aureus, persisters and biofilms, Synthetic Route of 72509-76-3, the main research area is felodipine aminoglycoside methicillin resistant Staphylococcus aureus biofilm; Aminoglycosides; Felodipine; Implant infection; Methicillin-resistant Staphylococcus aureus; Persisters.

Methicillin-resistant Staphylococcus aureus (MRSA), biofilms, and persisters are three major factors leading to recurrent and recalcitrant implant infections. Although antibiotics are still the primary treatment for chronic implant infections in clin., only few drugs are effective in clearing persisters and formed biofilms. Here, felodipine, a dihydropyridine calcium channel blocker, was reported for the first time to have antibacterial effects against MRSA, biofilm, and persisters. Even after continuous exposure to sub-lethal concentrations of felodipine, bacteria are less likely to develop resistance. Besides, low doses of felodipine enhances the antibacterial activity of gentamicin by inhibiting the expression of protein associated with aminoglycoside resistance (aacA-aphD). Next, biofilm eradication test and persisters killing assay suggested felodipine has an excellent bactericidal effect against formed biofilms and persisters. Furthermore, the result of protein profiling, and quant. metabonomics anal. indicated felodipine reduce MRSA virulence (agrABC), biofilm formation and TCA cycle. Then, mol. docking showed felodipine inhibit the growth of persisters by binding to the H pocket of ClpP protease, which could lead to substantial protein degradation Furthermore, murine infection models suggested felodipine in combination with gentamicin alleviate bacterial burden and inflammatory response. In conclusion, low dose of felodipine might be a promising agent for biomaterial delivery to enhance aminoglycosides efficacy against implant infections caused by MRSA, biofilm, and persisters.

Bioactive Materials published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Xinxin published the artcileDiltiazem inhibits SARS-CoV-2 cell attachment and internalization and decreases the viral infection in mouse lung, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is diltiazem antiviral agent cell attachment internalization SARS CoV2 infection.

The continuous emergence of severe acute respiratory coronavirus 2 (SARS-CoV-2) variants and the increasing number of breakthrough infection cases among vaccinated people support the urgent need for research and development of antiviral drugs. Viral entry is an intriguing target for antiviral drug development. We found that diltiazem, a blocker of the L-type calcium channel Cav1.2 pore-forming subunit (Cav1.2 α1c) and an FDA-approved drug, inhibits the binding and internalization of SARS-CoV-2, and decreases SARS-CoV-2 infection in cells and mouse lung. Cav1.2 α1c interacts with SARS-CoV-2 spike protein and ACE2, and affects the attachment and internalization of SARS-CoV-2. Our finding suggests that diltiazem has potential as a drug against SARS-CoV-2 infection and that Cav1.2 α1c is a promising target for antiviral drug development for COVID-19.

PLoS Pathogens published new progress about 28S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Catic-Djordjevic, Aleksandra published the artcileAssessment of pharmacokinetic mycophenolic acid clearance models using Monte Carlo numerical analysis, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is mycophenolic acid pharmacokinetics Monte Carlo simulation; Monte Carlo simulation; Mycophenolic acid; clearance; population pharmacokinetic analysis; renal transplant patients.

Previously, we performed population pharmacokinetic anal. and indicated age, mycophenolate mofetil (MMF)/mycophenolic acid (MPA) daily dose, and presence of nifedipine in patient therapy as significant predictors of MPA apparent clearance (CL/F) variability. This study aimed to determine the reliability of previously published population pharmacokinetic models derived from similar studies. Furthermore, this study investigated correspondence between chosen population models from the literature. By means of the Monte Carlo simulation method, pharmacokinetic models from different studies are simulated and analyzed in the range of standard deviations of measured system parameters as well as the range of observed model parameters taken from the comparison studies. The 1000 numerical simulations were performed for every analyzed model in order to calculate the most possible MPA CL/F values according to the expected values from the performed experiment Fitting our results with other models showed how the presence of nifedipine makes difference in MPA CL/F values. By testing the data from selected studies into our model, a similar range of expected CL/F values was obtained, which may confirm the validity of our model. The results of our population pharmacokinetic study are partially applicable in models by other researchers.

Xenobiotica published new progress about Albumins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mango, Katalin published the artcileCYP2B6 allelic variants and non-genetic factors influence CYP2B6 enzyme function, Related Products of pyridine-derivatives, the main research area is CYP2B6 allele genotype phenotype amoxicillin clavulanic acid cyclophosphamide.

Human CYP2B6 enzyme although constitutes relatively low proportion (1-4%) of hepatic cytochrome P 450 content, it is the major catalyst of metabolism of several clin. important drugs (efavirenz, cyclophosphamide, bupropion, methadone). High interindividual variability in CYP2B6 function, contributing to impaired drug-response and/or adverse reactions, is partly elucidated by genetic polymorphisms, whereas non-genetic factors can significantly modify the CYP2B6 phenotype. The influence of genetic and phenoconverting non-genetic factors on CYP2B6-selective activity and CYP2B6 expression was investigated in liver tissues from Caucasian subjects (N = 119). Strong association was observed between hepatic S-mephenytoin N-demethylase activity and CYP2B6 mRNA expression (P < 0.0001). In less than one third of the tissue donors, the CYP2B6 phenotype characterized by S-mephenytoin N-demethylase activity and/or CYP2B6 expression was concordant with CYP2B6 genotype, whereas in more than 35% of the subjects, an altered CYP2B6 phenotype was attributed to phenoconverting non-genetic factors (to CYP2B6-specific inhibitors and inducers, non-specific amoxicillin + clavulanic acid treatment and chronic alc. consumption, but not to the gender). Furthermore, CYP2B6 genotype-phenotype mismatch still existed in one third of tissue donors. In conclusion, identifying potential sources of CYP2B6 variability and considering both genetic variations and non-genetic factors is a pressing requirement for appropriate elucidation of CYP2B6 genotype-phenotype mismatch. Scientific Reports published new progress about Alcohols Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yuan, Zi-Qing-Yun published the artcileImpact of 14 types of genetic polymorphisms on antihypertensive efficacy of felodipine in healthy Chinese subjects, Product Details of C18H19Cl2NO4, the main research area is felodipine genetic polymorphism antihypertensive efficacy.

This study evaluated different influences of 14 single nucleotide polymorphisms (SNPs) and demog. factors leading to individual differences in the antihypertensive efficacy of felodipine in healthy Chinese subjects. 24 Subjects were sequenced for candidate SNPs. Plasma samples were obtained as clin. trial protocol, and were determined by a HPLC-MS/MS method. Pharmacokinetic parameters were calculated by WinNonlin 6.0. Statistical anal. was mainly performed by SPSS 22.0. A multiple linear regression model provided different weight coefficients of different demog. and genetic factors. The trend of Cmax is almost consistent with AUCss increase, but tmax of individuals is different; the antihypertensive effect of felodipine is individually different. A significant association was observed between systolic blood pressure decrease (δSBP) and SNPs of CACNA1C, CACNA1D, GNB3 resp., while CACNA1C and CACNA1 were associated with diastolic blood pressure decrease (δDBP). CYP3A5 rs766746 and CYP3A4 rs2242480 were linked with Cmax and AUCss, and ABCB1 rs1045642 was associated with T1/2. Significant relationships were shown between AUCss and ΔSBP (p = 0.022) as well as Cmax and ΔSBP (p = 0.015). The efficacy of felodipine is individually different, influenced especially by CACNA1C rs1051375 and ABCB1 rs1045642. δDBP is associated with δSBP in multiple-dosing of felodipine in healthy Chinese subjects.

International Journal of Clinical Pharmacology and Therapeutics published new progress about Antihypertensives. 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

Drumm, Bernard T. published the artcileCa2+ signaling in interstitial cells of Cajal contributes to generation and maintenance of tone in mouse and monkey lower oesophageal sphincters, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is calcium Cajal interstitial cell tone lower oesophageal sphincter signaling; Ca2+ handling mechanisms; L-type Ca2+ channels; SIP syncytium; anoctamin-1 channels; oesophageal reflux; smooth muscle cells; swallowing reflex.

The lower oesophageal sphincter (LES) generates tone and prevents reflux of gastric contents. LES smooth muscle cells (SMCs) are relatively depolarised, facilitating activation of Cav1.2 channels to sustain contractile tone. We hypothesised that i.m. interstitial cells of Cajal (ICC-IM), through activation of Ca2+-activated Cl- channels (ANO1), set membrane potentials of SMCs favorable for activation of Cav1.2 channels. In some gastrointestinal muscles, ANO1 channels in ICC-IM are activated by Ca2+ transients, but no studies have examined Ca2+ dynamics in ICC-IM within the LES. Immunohistochem. and qPCR were used to determine expression of key proteins and genes in ICC-IM and SMCs. These studies revealed that Ano1 and its gene product, ANO1, are expressed in c-Kit +cells (ICC-IM) in mouse and monkey LES clasp muscles. Ca2+ signalling was imaged in situ, using mice expressing GCaMP6f specifically in ICC (Kit-KI-GCaMP6f). ICC-IM exhibited spontaneous Ca2+ transients from multiple firing sites. Ca2+ transients were abolished by cyclopiazonic acid or caffeine but were unaffected by tetracaine or nifedipine. Maintenance of Ca2+ transients depended on Ca2+ influx and store reloading, as Ca2+ transient frequency was reduced in Ca2+ free solution or by Orai antagonist. Spontaneous tone of LES muscles from mouse and monkey was reduced �0% either by Ani9, an ANO1 antagonist or by the Cav1.2 channel antagonist nifedipine. Membrane hyperpolarisation occurred in the presence of Ani9. These data suggest that intracellular Ca2+ activates ANO1 channels in ICC-IM in the LES. Coupling of ICC-IM to SMCs drives depolarisation, activation of Cav1.2 channels, Ca2+ entry and contractile tone.

Journal of Physiology (Oxford, United Kingdom) published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Gja7). 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