Category: 21829-25-4

Hawlitschek, Christina published the artcileAntihypertensive and cardioprotective effects of different monotherapies and combination therapies in young spontaneously hypertensive rats – A pilot study, Product Details of C17H18N2O6, the publication is Saudi Journal of Biological Sciences (2022), 29(1), 339-345, database is CAplus and MEDLINE.

Spontaneously hypertensive rats (SHR) are an established animal model for antihypertensive treatment. The aim of this pilot study was a systematic search for two lines of antihypertensive treatment – a monotherapy and a combination of two drugs – to be applied in a future study on old SHR. Originally, representatives of three drug classes recommended for antihypertensive therapy in humans should be applied, namely captopril (CAP) as an antagonist of the renin-angiotensin-aldosterone system, nifedipine (NIF) as calcium channel blocker and propranolol (PROP) as β-adrenergic blocker. As we observed that PROP had been poorly ingested, all groups with PROP therapy were excluded from the study. CAP (60 mg kg^-1 d^-1), NIF (10 mg kg^-1 d^-1) or both were administered orally to seven-week-old SHR over 3 wk. A further group of SHR received no treatment (SHR/CTRL). Age-matched normotensive Wistar-Kyoto rats served as normotensive controls. We examined the effect of the antihypertensive therapies on systolic blood pressure, heart weight and on histol. and biochem. markers of cardiac hypertrophy and fibrosis. CAP proved to be the most effective treatment reducing blood pressure and relative heart weight significantly compared to SHR/CTRL without reaching normotensive values. Beginning cardiac fibrosis observed in SHR/CTRL was completely abrogated with CAP treatment. Similar effects were achieved with a combination of CAP and NIF. CAP as monotherapy and CAP + NIF as combination therapy were chosen for the forthcoming study on old SHR.

Saudi Journal of Biological Sciences 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

Yao, Xin published the artcileSurfactants Accelerate Crystallization of Amorphous Nifedipine by Similar Enhancement of Nucleation and Growth Independent of Hydrophilic-Lipophilic Balance, Computed Properties of 21829-25-4, the publication is Molecular Pharmaceutics (2022), 19(7), 2343-2350, database is CAplus and MEDLINE.

Amorphous formulations, increasingly employed to deliver poorly soluble drugs, generally contain surfactants to improve wetting and dissolution These surfactants are often liquids and can potentially increase the mobility of the drug and reduce its stability, but little is known about this effect. Here we investigate the effect of four common nonionic surfactants (Tween 80, Span 80, Triton X-100, and Poloxamer 407) on the crystallization of amorphous nifedipine (NIF). We find that the surfactants significantly enhance the rates of crystal nucleation and growth even at low concentrations, by up to 2 orders of magnitude at 10 wt %. The surfactants tested show similar enhancement effects independent of their structural details and hydrophilic-lipophilic balance (HLB), suggesting that surfactant adsorption at solid/liquid interfaces does not play a major role in crystal nucleation and growth. Importantly, the surfactants accelerate crystal nucleation and growth by a similar factor. This result mirrors the previous finding that a polymer dopant in a mol. glass-former causes similar slowdown of nucleation and growth. These results indicate that nucleation and growth in a deeply supercooled liquid are both mobility-limited, and a dopant mainly functions as a mobility modifier (enhancer or suppressor depending on the dopant). The common surfactants tested are all mobility enhancers and destabilize the amorphous drug, and this neg. effect must be managed using stabilizers such as polymers. The effect of surfactants on nucleation can be predicted from the effect on crystal growth and the crystallization kinetics of the pure system, using the same principle previously established for drug-polymer systems. We show how the independently measured nucleation and growth rates enable predictions of the overall crystallization rates.

Molecular Pharmaceutics 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 C9H7NO2, Computed Properties of 21829-25-4.

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

Lazcano-Perez, Fernando published the artcileA Sea Anemone Lebrunia neglecta Venom Fraction Decreases Boar Sperm Cells Capacitation: Possible Involvement of HVA Calcium Channels, Computed Properties of 21829-25-4, the publication is Toxins (2022), 14(4), 261, database is CAplus and MEDLINE.

Sea anemones produce venoms characterized by a complex mixture of low mol. weight compounds, proteins and peptides acting on voltage-gated ion channels. Mammal sperm cells, like neurons, are characterized by their ion channels. Calcium channels seem to be implicated in pivotal roles such as motility and capacitation. In this study, we evaluated the effect of a low mol. weight fraction from the venom of the sea anemone Lebrunia neglecta on boar sperm cells and in HVA calcium channels from rat chromaffin cells. Spermatozoa viability seemed unaffected by the fraction whereas motility and sperm capacitation were notoriously impaired. The sea anemone fraction inhibited the HVA calcium current with partial recovery and no changes in chromaffin cells’ current kinetics and current-voltage relationship. These findings might be relevant to the pharmacol. characterization of cnidarian venoms and toxins on voltage-gated calcium channels.

Toxins 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, Computed Properties of 21829-25-4.

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

Gawri, Rahul published the artcileThe anabolic effect of inorganic polyphosphate on chondrocytes is mediated by calcium signalling, Synthetic Route of 21829-25-4, the publication is Journal of Orthopaedic Research (2022), 40(2), 310-322, database is CAplus and MEDLINE.

Inorganic polyphosphates (polyP) are polymers composed of phosphate residues linked by energy-rich phosphoanhydride bonds. As polyP can bind calcium, the hypothesis of this study is that polyP enters chondrocytes and exerts its anabolic effect by calcium influx through calcium channels. PolyP treatment of cartilage tissue formed in 3D culture by bovine chondrocytes showed an increase in proteoglycan accumulation but only when calcium was also present at a concentration of 1.5 mM. This anabolic effect could be prevented by treatment with either ethylene glycol-bis(β-aminoethyl ether)-N,N,N,N-tetraacetic acid or the calcium channel inhibitors gadolinium and nifedipine. Calcium and polyP cotreatment of chondrocytes in monolayer culture resulted in calcium oscillations that were polyP chain length specific and were inhibited by gadolinium and nifedipine. The calcium influx resulted in increased gene expression of sox9, collagen type II, and aggrecan which was prevented by treatment with either calphostin, an inhibitor of protein kinase C, and W7, an inhibitor of calmodulin; suggesting activation of the protein kinase C-calmodulin pathway. Tracing studies using 4,6-diamidino-2-phenylindole, Mitotracker Red, and/or Fura-AM staining showed that polyP was detected in the nucleus, mitochondria, and intracellular vacuoles suggesting that polyP may also enter the cell. PolyP colocalizes with calcium in mitochondria. This study demonstrates that polyP requires the influx of calcium to regulate chondrocyte matrix production, likely via activating calcium signaling. These findings identify the mechanism regulating the anabolic effect of polyP in chondrocytes which will help in its clin. translation into a therapeutic agent for cartilage repair.

Journal of Orthopaedic 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, Synthetic Route of 21829-25-4.

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

Peeters, Laura E. J. published the artcileDevelopment and Validation of a Dried Blood Spot Assay Using UHPLC-MS/MS to Identify and Quantify 12 Antihypertensive Drugs and 4 Active Metabolites: Clinical Needs and Analytical Limitations, Formula: C17H18N2O6, the publication is Therapeutic Drug Monitoring (2022), 44(4), 568-577, database is CAplus and MEDLINE.

As nonadherence to antihypertensive drugs (AHDs) can increase the risk of cardiovascular events, hospitalization, and higher costs, there is a need for a reliable, objective, and easy method to assess nonadherence in patients. The dried blood spot (DBS) sampling method used to measure drug concentrations meets these requirements. For detecting nonadherence, identification is more important than quantification. Owing to their use in clin. practice, it is important to measure multiple AHDs with a single method. Therefore, we developed and validated a single DBS method for 17 commonly used AHDs and 4 active metabolites using ultrahigh performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS). Anal. validation of the DBS assay was performed in accordance with the guidelines on bioanal. method validation of the European Medicines Agency and US Food and Drug Administration as well as the International Association of Therapeutic Drug Monitoring and Clin. Toxicol. guidelines. We validated 12 of the 17 AHDs according to the European Medicines Agency and Food and Drug Administration requirements for bioanal. method validation. Eleven AHDs were validated for both identification and quantification of drug concentrations, whereas nifedipine was only validated for identification. However, 5 of the 17 AHDs were excluded due to suboptimal validation results. Lercanidipine was excluded due to nonlinearity, and all 4 AHDs measured in the neg. mode of UHPLC-MS/MS were not in accordance with one or more of the acceptance criteria and were therefore excluded. The described method accurately measured AHDs in DBS and can be used to determine nonadherence in patients. However, method validation revealed a challenging balance between anal. limitations and clin. needs when analyzing multiple drugs using the same method.

Therapeutic Drug Monitoring 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, Formula: C17H18N2O6.

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

Teimouri, Arezou published the artcileStability of Compounded Topical Nifedipine in Cream, Gel, and Ointment Bases., HPLC of Formula: 21829-25-4, the main research area is .

The objective of this study was to investigate the stability of compounded nifedipine cream in gel and ointment formulations dispensed in white plastic and glass amber jars. Extemporaneously compounded nifedipine cream (Glaxal Base), gel (K-Y Jelly), and ointment (Aquaphor) in white plastic and glass amber jars were stored at 4°C, 23°C, and 40°C. We determined potency on days 0, 7, 14, 30, 60, and 90, and subsequently assigned beyond-use-dates based on United States Pharmacopeia recommendations, organoleptic properties, and pH changes. Nifedipine potency in cream and ointment stored in white plastic jars was within ±10% of initial for 90 days (excluding day 14 for cream). In glass amber jars, potency was outside the acceptable range by day 14 at 23°C but within range for 90 days at 4°C (excluding day 30). Nifedipine potency was maintained for 90 days in both jars at 23°C and 4°C (excluding day 30) and in white plastic jars at 40°C, but 60 days stored in glass amber jars. The pH of formulations was stable with changes of less than 1-unit pH. At 40°C, a significant decrease in apparent viscosity of cream was evident on day 90. There was a decrease in apparent viscosity and phase separation of the ointment at 40°C and an increase in apparent viscosity (difficult to mix) at 4°C on day 14 onwards. Significant organoleptic changes were observed by day 7 at 40°C (decrease in apparent viscosity and abnormal odor by day 90), day 30 at 4°C (thicker consistency), and day 90 at 23°C (abnormal odor). Storage in white plastic jars at 23°C is recommended for compounded topical nifedipine cream and ointment (for 90 days), and for gel (60 days).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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

Teimouri, Arezou published the artcileDrug-release Assessment of Compounded Topical Nifedipine and Diltiazem in Commonly Used Bases for Wound Healing., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is .

The objective of this study was to determine release profiles of extemporaneously compounded nifedipine and diltiazem in commonly used bases in pharmacy practice. Release of nifedipine 0.2%, 2%, and 10% (w/w) from Glaxal Base, K-Y Jelly, and Aquaphor Healing Ointment, and of diltiazem 2% (w/w) from GlaxalBase, hydroxyethyl cellulose-based gel, and white petrolatum was quantified using the Franz-cell diffusion system. The cumulative release was determined at 0.5 hour, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, and 6 hours. Two-way ANOVA with Tukey’s posthoc test was used for statistical analyses, with a P-value of <0.05 considered significant. At a 0.2% concentration, cumulative nifedipine release was highest from Glaxal Base. At 2% and 10% concentrations, nifedipine release was highest from K-Y Jelly, although this was only significantly different from Glaxal Base at 6 hours and 1.5 hours, 4 hours, 6 hours (P<0.05), respectively. Diltiazem release from Glaxal Base and white petrolatum was significantly lower than the gel (P<0.05). No significant difference in diltiazem release from Glaxal Base at 0.5 hour was observed versus white petrolatum (P>0.05). Nifedipine and diltiazem release both followed Higuchi’s mathematical model with the highest coefficient of determination (R2) for all formulations. Of the bases studies, Glaxal Base is the recommended base for compounding topical nifedipine (0.2%). For higher concentrations of nifedipine (2% and10%), both Glaxal Base and K-Y Jelly are suitable options for base selection. A hydroxyethylcellulose-based gel is recommended for topical diltiazem (2%).

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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

Riepl, Mike published the artcileA Compendium of Compounding Agents and Formulations, Part 4: Nifedipine and Pentoxifylline., Category: pyridine-derivatives, the main research area is .

The medical, economic, and social effects of painful chronic wounds such as anal fissures, which frequently prove refractory to treatment with commercially available medications, are often underestimated by clinicians. Those types of injuries, which afflicted individuals are often reluctant to discuss with healthcare providers, can lead to a greatly restricted lifestyle; result in depression, anxiety, social isolation, and embarrassment; require extended or repeated hospital stays; and create a financial burden for the patient and for society. Because interpatient variables can preclude the effectiveness of standardized mass-produced wound-healing products, a compounded formulation that can be formulated to include drugs proven effective in safe but off-label uses and that can be modified as patients’ medical needs require may achieve the therapeutic goal. In this report, 2 such agents shown to promote wound healing are profiled: the vasodilator nifedipine, a first-generation calcium channel blocker that is used to treat hypertension and angina pectoris; and pentoxifylline, a synthetic dimethylxanthine derivative that facilitates vasodilation, improves erythrocyte flexibility, enhances blood flow, and reduces blood viscosity. Formulations that incorporate those drugs, which are underrecognized as effective healing agents when compounded as directed, are included for easy reference.

International journal of pharmaceutical compounding published new progress in MEDLINE about 21829-25-4, 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

Wu, Y published the artcileRegulation of magnesium sulfate combined with nifedipine and labetalol on disease-related molecules in serum and placenta in the treatment of preeclampsia., HPLC of Formula: 21829-25-4, the main research area is .

OBJECTIVE: To explore the regulatory effect of magnesium sulfate combined with nifedipine and labetalol on disease-related molecules in serum and placenta in the treatment of preeclampsia. PATIENTS AND METHODS: Altogether 100 patients with preeclampsia admitted to the Children & Women’s Healthcare of Laiwu City were selected. They were divided into control group and experimental group according to different treatment methods. Among them, 51 patients in the control group were treated with magnesium sulfate combined with nifedipine, and 49 patients in the experimental group were treated with labetalol on the basis of the treatment in the control group. The therapeutic effects of the two methods were compared. The levels of the following factors in the two groups were compared: kallikrein expression, pregnancy-associated plasma protein A (PAPP-A), pregnancy-specific β1 glycoprotein (SPI), placental growth factor (PLGF), human placental prolactin (HPL), transforming growth factor β1(TGF-β1), vascular cell adhesion molecule 1 (VCAM-1) and E-selectin in serum and placenta tissues. RESULTS: After treatment, the blood pressure in the experimental group was lower than that in the control group (p<0.05). The expression of kallikrein in serum and placental tissue of the patients in the experimental group was higher than that of the patients in the control group (p<0.05); PAPP-A level was lower than that in the control group (p<0.05); TGF-β1 level was higher than that in the control group (p<0.05); VCAM-1 and E-selectin were lower than those in the control group (p<0.05), and kallikrein and TGF-β1 in serum and placenta in the non-occurrence group were higher than those in the occurrence group (p<0.05). The serum and placenta PAPP-A, VCAM-1, and E-selectin in the non-occurrence group were lower than those in the occurrence group (p<0.05). CONCLUSIONS: Magnesium sulfate combined with nifedipine and labetalol has good efficacy in the treatment of preeclampsia. They can promote the expression of endogenous kallikrein, reduce the level of pregnancy-related hypertension predictors, and weaken the infiltration ability of cytotrophoblasts. European review for medical and pharmacological sciences published new progress in MEDLINE about 21829-25-4, 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

Zhang, Zhenzhen published the artcileCase Report: Optical Coherence Tomography Can Find Typical Features in Pregnancy-induced Hypertension with Retinopathy., Quality Control of 21829-25-4, the main research area is .

SIGNIFICANCE: Pregnancy-induced hypertension is a unique yet common complication in pregnant women and may cause retinopathy. Optical coherence tomography (OCT) may help find the features of retinopathy that are difficult to observe through fundus examination. Not all patients can fully recover from retinopathy. PURPOSE: This report describes a case of pregnancy-induced hypertension with retinopathy and represents the features of retinopathy in OCT and fundus fluorescein angiography. CASE REPORT: A 29-year-old pregnant woman presented with bilateral blurred vision and xanthopsia 2 days before her induced labor; she was also diagnosed as pre-eclamptic in the obstetrics department. The vision in her right eye was 20/33, and that in her left eye was 20/20. Fundus fluorescein angiography showed scattered-dot hypofluorescence around the disc at an early stage, and needle-like hyperfluorescence gradually appeared near the disc with late-stage fluorescein leakage in both eyes. Optical coherence tomography revealed multiple shallow retinal detachments with hyperreflective bright spots in the outer retina and clumped hyperreflective materials on the retinal pigment epithelium (RPE). CONCLUSIONS: Typical findings and some tiny changes in the outer retina and RPE can be observed through spectral-domain OCT. The clumped hyperreflective deposits in the outer retina may be by-products of RPE swelling and necrosis that lead to barrier dysfunctions and fluid leakage. These described features may help diagnose retinopathy from pregnancy-induced hypertension. Although it is a self-limited disease, the disruptions in the ellipsoid and interdigitation zones may not fully recover and result in reduced visual dysfunction. Therefore, control of hypertension is indicated.

Optometry and vision science : official publication of the American Academy of Optometry published new progress in MEDLINE about 21829-25-4, 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