Tag: M.W=200-350

Archana, G. M. published the artcileAssays for L-type voltage gated calcium channels, Synthetic Route of 21829-25-4, the main research area is Calcium imaging; Drug discovery; End-point assay for calcium channel; HEK-293; L-type voltage gated calcium channel; VGCC assay.

Voltage gated calcium channels (VGCCs) are pursued as drug targets for neurodegenerative and cardiovascular diseases. High throughput drug screening targeting VGCCs depends on patch-clamp electrophysiol. or fluorophore-based calcium imaging that requires powerful equipment and specialized expertise thus leading to cost escalation. Moreover, VGCC needs to be transfected into cell lines such as HEK-293. We report the presence of L-type VGCC (L-VGCC) subunit proteins, Cav1.2, α2δ and β in HEK-293 cells and the application of simple methods for its assay. Endogenous expression of the channel in HEK-293 cells overcomes the need for transfection. L-VGCC in HEK-293 cells was activated either by the agonist, BayK8644 or by KCl-mediated depolarization. Activity was detected using the calcium sensing probe, GCaMP6m by live imaging. L-VGCC activity induced enhancement in GCaMP6m fluorescence returned to baseline corresponding to channel-closure. Activity was also shown using a methodol. involving end-point detection of the calcium dependent interaction of α-CaMKII with NMDA receptor subunit GluN2B sequence. This methodol. further simplifies the assay as it eliminates the need for real time imaging. Activation was blocked by the specific L-type VGCC antagonist, nifedipine. Finding the protein and activity of L-VGCC in HEK-293 cells offers com. viable assays for drug screening.

Analytical Biochemistry published new progress about Calcium imaging; Drug discovery; End-point assay for calcium channel; HEK-293; L-type voltage gated calcium channel; VGCC assay. 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

Engin, Seckin published the artcileThe inhibitory effect of trimetazidine on detrusor contractility – a potential repositioning of trimetazidine for the treatment of overactive bladder., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is calcium; detrusor; fura-2; ion channels; isolated tissue bath; trimetazidine.

OBJECTIVES: This study aimed to identify the effect of trimetazidine (TMZ), an antianginal drug, on detrusor smooth muscle (DSM) contractility and its possible mechanisms of action. METHODS: We performed in-vitro contractility studies on isolated mouse DSM strips and investigated the effect of TMZ on Ca2+ levels in fura-2-loaded A7r5 cells. KEY FINDINGS: TMZ (300 or 1000 µM) inhibited carbachol (CCh)- and KCl-induced contractions and produced a concentration-dependent (10-1000 µM) relaxation in KCl-precontracted DSM strips. TMZ-induced relaxation was markedly decreased by BaCl2, an inward-rectifying K+ channel blocker, but was not altered by preincubation with tetraethylammonium, glibenclamide, 4-aminopyridine, propranolol, L-NAME or methylene blue. TMZ (300 or 1000 µM) reduced both the CaCl2-induced contraction of depolarized DSM strips under Ca2+-free conditions and the CCh-induced contraction of DSM strips preincubated with nifedipine in Ca2+-containing Krebs solution. Furthermore, TMZ (1000 µM) significantly decreased the Ca2+ levels in fura-2-loaded A7r5 cells. CONCLUSIONS: TMZ decreased DSM contractility and caused a concentration-dependent relaxation of the tissue possibly through its actions on Ca2+ transients and K+ channels. Our results provide preclinical evidence that TMZ would be a potential candidate to treat disorders related to the overactivity of the bladder.

The Journal of pharmacy and pharmacology published new progress about calcium; detrusor; fura-2; ion channels; isolated tissue bath; trimetazidine. 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

Yuan, Yanbing published the artcileRapid detection of illegally added nifedipine in Chinese traditional patent medicine by surface-enhanced Raman spectroscopy., Product Details of C17H18N2O6, the main research area is Chinese traditional patent medicine; Illegal addition; Nanoparticles; Nifedipine; Surface-enhanced Raman spectroscopy.

Nifedipine is an antihypertensive chemical. The illegal addition of this chemical into Chinese traditional patent medicine (CTPM) is unstandardized and lacks regulation. It could bring serious side effects to patients, causing various symptoms. Therefore, accurate detection of nifedipine is very important for human health and the prevention of illegal additives. Surface-enhanced Raman spectroscopy (SERS) is a fast and sensitive fingerprint spectroscopic technique, which has been shown to be promising in drug detection. In this study, nifedipine in CTPM was determined qualitatively and quantitatively with SERS. Linear relationships between the concentrations of nifedipine and the intensities of the characteristic peaks were established. The results showed a linear relationship within the concentration range of 0.5-10 mg/L, and the lowest detectable concentration of nifedipine in CTPM was 0.1 mg/L (equivalent to 0.03% doping of nifedipine in CTPM). This method has shown a great potential in the detection of drugs illegally added to CTPM.

Analytical sciences : the international journal of the Japan Society for Analytical Chemistry published new progress about Chinese traditional patent medicine; Illegal addition; Nanoparticles; Nifedipine; Surface-enhanced Raman spectroscopy. 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

Salama, Mohamed published the artcileMethyldopa versus nifedipine or no medication for treatment of chronic hypertension during pregnancy: A multicenter randomized clinical trial., Application In Synthesis of 21829-25-4, the main research area is Chronic hypertension; Fetal outcome; Maternal outcome; Methyldopa; Nifedipine.

OBJECTIVE: To assess the maternal and fetal outcome in women with mild to moderate chronic hypertension on antihypertensive drug (methyldopa or nifedipine) therapy compared to no medication. METHODS: This multicenter randomized clinical trial was conducted at Menoufia University hospital, Shibin El-kom Teaching hospital and 11 Central hospitals at Menoufia governorate, Egypt.490 pregnant women with mild to moderate chronic hypertension were randomized into three groups; methyldopa group (n��66), nifedipine group (n��60) and control or no medication group (n��64) who were followed from the beginning of pregnancy till the end of puerperium to record maternal and fetal outcome. RESULTS: Mothers in the control (no medication) group were more prone for the development of severe hypertension, preeclampsia, renal impairment, ECG changes, placental abruption and repeated hospital admissions (p��.001) when compared to mothers in both treatment groups (methyldopa and nifedipine). Neonates in the control (no medication) group were more prone for prematurity and admission to neonatal ICU (p��.001). CONCLUSION: Antihypertensive drug therapy is advisable in mild to moderate chronic hypertension during pregnancy to decrease maternal and fetal morbidity. When considering which agents to use for treatment, oral methyldopa and nifedipine are valid options.

Pregnancy hypertension published new progress about Chronic hypertension; Fetal outcome; Maternal outcome; Methyldopa; Nifedipine. 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

Wakabayashi, Kohei published the artcileAcute myocardial infarction caused by persistent coronary spasm associated with high-grade macrophage accumulation., Category: pyridine-derivatives, the main research area is clinical diagnostic tests; ischaemic heart disease.

The mechanisms responsible for persistent and lethal coronary spasm remain incompletely understood. Our group treated a patient with non-ST-elevation myocardial infarction (MI) caused by a spontaneously persistent spasm associated with high-grade macrophage accumulation. A 48-year-old man was transferred to an emergency room because of persisted chest tightness. The patient’s chest pain subsided without ST elevation when he arrived at the hospital, but he tested positive for fatty acid-binding protein. Emergent coronary angiography revealed a subtotal occlusion in the middle of the right coronary artery. The occluded lesion was released immediately after an injection of isosorbide dinitrate. No disruption, ulceration or erosion was observed at the culprit lesion segment on optical coherence tomography. The only finding was high-grade macrophage accumulation in the segment of the persistent focal coronary spasm. The present case suggests that the early stage of atherosclerosis with high-grade macrophage accumulation was associated with persistent coronary spasm resulting in acute MI.

BMJ case reports published new progress about clinical diagnostic tests; ischaemic heart disease. 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

Wang, Pengfei published the artcileThe fingerprints of nifedipine/isonicotinamide cocrystal polymorph studied by terahertz time-domain spectroscopy, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Cocrystal polymorph; Nifedipine; Quantum chemical calculations; Spectral fingerprints; Terahertz time-domain spectroscopy; Vibrational modes.

Cocrystal is constructed to improve physicochem. properties of active pharmaceutical ingredient and prevent polymorphism via intermol. interactions. However, recent examples on cocrystal polymorphs display significantly different properties. Even though some anal. techniques have been used to characterize the cocrystal polymorphic system, it remains unclear how intermol. interactions drive and stabilize the structure. In this work, we study the cocrystal polymorphs of nifedipine (NFD) and isonicotinamide (INA) using terahertz (THz) spectroscopy. Form I and form II of NFD-INA cocrystals show spectral fingerprints in THz region. Temperature-dependent THz spectra display distinguished frequency shifts of each fingerprint. Combined with solid-state d. functional theory (DFT) calculations, the exptl. fingerprints and their distinct responses to temperature are elucidated by specific collective vibrational modes. The vibrations of hydrogen bonding between dihydropyridine ring of NFD and INA are generally distributed below 1.5 THz, which play important roles in stabilizing cocrystal and preventing the oxidation of NFD. The rotations of Me group in NFD are widely distributed in the range of 1.5-4.0 THz, which helps the steric recognition. The results demonstrate that THz spectroscopy is a sensitive tool to discriminate cocrystal polymorphs. It has the potential to be used as a non-invasive technique for pharmaceutical screening.

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about Cocrystal polymorph; Nifedipine; Quantum chemical calculations; Spectral fingerprints; Terahertz time-domain spectroscopy; Vibrational modes. 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

Campochiaro, Corrado published the artcileAutoimmunity and immunodeficiency at the crossroad: autoimmune disorders as the presenting feature of selective IgM deficiency., HPLC of Formula: 21829-25-4, the main research area is connective tissue disease; immunology.

Selective immunoglobulin M deficiency (sIgMD) is an immunodeficiency with undefined pathogenesis and commonly presenting with recurrent infections. 1 The European Society for Immunodeficiencies Registry defines sIgMD as a serum IgM level repeatedly below 2 SD of normal with normal levels of serum IgA, IgG and IgG subclasses, normal vaccination responses, absence of T-cell defects and absence of causative external factors. Rarely it can also be associated with autoimmune diseases. 2-7 Here we describe a patient with primary sIgMD; who presented with multiple autoimmune diseases without a history of recurrent infections and we provide a short literature review on sIgMD and autoimmune diseases.

BMJ case reports published new progress about connective tissue disease; immunology. 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

Ibrahim, Mohammed H. published the artcileThe effectiveness of nifedipine/indomethacin combination therapy and nifedipine monotherapy for postponing preterm birth (25-34 weeks of gestation) in Sudanese women: a randomized clinical trial study protocol, SDS of cas: 21829-25-4, the main research area is Control trial; Indomethacin; Nifedipine; Preterm labor; Tocolytics.

Abstract: Background: Preterm birth is the most common cause of neonatal morbidity and mortality. Tocolytics are considered a standard treatment for women with threatened preterm delivery to allow time for maternal steroid administration and transfer to referral centers with neonatal intensive care units. However, there is controversy about the best tocolytic therapy to be considered as the first choice. The aim of this study is to compare the tocolytic effectiveness and tolerability of combination therapy with nifedipine and indomethacin vs. nifedipine monotherapy among Sudanese women with preterm labor (PTL) as well as to compare the possible neonatal outcomes associated with each drug. Methods/design: This is a randomized controlled clin. trial to be conducted in the Medani Maternity Hospital, Sudan. Women aged 18-40 years that are diagnosed with preterm labor and have a gestational age between 25 and 34 wk will be eligible to participate in this trial. The diagnosis of threatened PTL is defined as persistent uterine contractions “”(four contractions every 20 min or eight contractions every 60 min)”” with cervical changes “”(cervical effacement â‰?0% or cervical dilatation >two cm)””. Patients will be eligible regardless of the presentation of the fetus. It will be randomly decided whether participants receive nifedipine/indomethacin combination therapy or nifedipine monotherapy. The primary outcome is the number of women who do not deliver and do not need alternative tocolytic drug (terbutaline). The secondary outcome is an estimated association with neonatal morbidity and mortality. The sample size will be 117 subjects in each arm of the study, according to a type I error of 0.05 and a study power of 80%. Discussion: We expect higher effectiveness of the combination indomethacin/nifedipine tocolytic therapy compared with nifedipine monotherapy. We plan to suggest this combination therapy as the best option for postponing PTL. Trial registration: Clin. trial registration: PACTR202004681537890, date of registration: March 8, 2020.

BMC Pregnancy and Childbirth published new progress about Control trial; Indomethacin; Nifedipine; Preterm labor; Tocolytics. 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

Teragawa, Hiroki published the artcileThe Significance of Recognizing Myocardial Bridge in the Coronary Spasm Diagnosis in Myocardial Infarction with Nonobstructive Coronary Arteries., Product Details of C17H18N2O6, the main research area is coronary spasm; myocardial bridge; myocardial infarction with nonobstructive coronary arteries; vasospastic angina.

A 61-year-old man experienced chest oppression for 1 hour. He was positive for troponin T and underwent emergent coronary angiography (CAG), which did not reveal significant coronary stenosis. He was diagnosed with myocardial infarction with nonobstructive coronary arteries (MINOCA). We performed a spasm-provocation test, which revealed a focal spasm at the segment of the myocardial bridge. After receiving a calcium-channel blocker, he exhibited a good clinical course. Coronary spasm is considered an underlying cause of MINOCA; therefore, the presence of a myocardial bridge may help with the diagnosis.

Internal medicine (Tokyo, Japan) published new progress about coronary spasm; myocardial bridge; myocardial infarction with nonobstructive coronary arteries; vasospastic angina. 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

Gao, Zongming published the artcileAn In Vitro Dissolution Method for Testing Extended-Release Tablets Under Mechanical Compression and Sample Friction, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Critical quality attributes (CQAs); Extended-release (ER); Gastrointestinal (GI) condition; In vitro dissolution testing; Mechanical apparatus under GI condition (MAGIC) system; Medium flow-through configuration; Simulated GI compression and friction.

The release and dissolution of an active pharmaceutical ingredient (API) from the solid oral formulation into the gastrointestinal (GI) tract is critical for the drug′s absorption into systemic circulation. Extended-release (ER) solid oral dosage forms are normally subjected to phys. shear and grinding forces as well as pressure exerted by peristaltic movements when passing through the GI tract. The complex phys. contraction and sample friction exerted by the GI tract are not simulated well by compendial dissolution methods. These limitations render traditional in vitro dissolution testing unable to discriminate and predict a product′s in vivo performance. The objective of this study was to develop a dissolution method that better simulates the GI environment that products are subject to when taken by patients. A newly designed Mech. Apparatus under GI Conditions (MAGIC) was assembled with a dissolution platform and mech. capabilities to allow in vitro dissolution testing under sample contractions and friction. The dissolution platform, with medium flow-through configuration, was manufactured by 3D printing. A 60 mg polymer matrix-based ER nifedipine product was tested. To simulate GI physiol. conditions during the dissolution testing, the flow rate of the medium, and a combination of mech. compression with rotation induced sample friction at various rotation frequencies were explored. The polymer matrix-based nifedipine ER formulation used here failed its controlled release functionality in the simulated GI environment under mech. compression and sample friction. The results showed that the MAGIC system, with flow-through configuration under compression and sample friction, has advantages over compendial methods in testing ER solid oral formulations.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Critical quality attributes (CQAs); Extended-release (ER); Gastrointestinal (GI) condition; In vitro dissolution testing; Mechanical apparatus under GI condition (MAGIC) system; Medium flow-through configuration; Simulated GI compression and friction. 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