Tag: M.W=300-350

Safarudin published the artcileEvaluation of lipid profile in patients with cardiovascular diseases receiving simvastatin in Palu Indonesia, Related Products of pyridine-derivatives, the publication is Journal of Pharmacy and Nutrition Sciences (2018), 8(4), 199-204, database is CAplus.

Cardiovascular diseases (CVDs) are the leading cause of death worldwide which results from the impaired function of the heart and blood vessels. The most common CVDs are coronary heart and stroke. The main clin. manifestation of these diseases is the formation of atherosclerosis which is associated with the change of blood lipid levels. Simvastatin is widely used in patients with impaired lipid levels in the blood. The study was a descriptive research with a retrospective approach on medical record data (n = 64) taken from Palu City, Central Sulawesi, Indonesia. The variables included in this study were gender, age, diagnosis, co-medication, lipid profile including total cholesterol, LDL, triglycerides, and HDL in patients with CVDs receiving simvastatin. In the study, sixty-four patients of CVDs met the inclusion and exclusion criteria. This study suggested that simvastatin achieved to normalize the blood lipid levels, including total cholesterol in forty-four patients (68.75%), LDL in forty-nine patients (80.3%), triglycerides in fifty-nine patients (92.19%), and HDL in fifty-two patients (81.25%). The use of simvastatin in patients with CVDs managed to lower total cholesterol, LDL, and triglycerides, as well as increase the HDL level.

Journal of Pharmacy and Nutrition Sciences published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C10H20N2O6S2, Related Products of pyridine-derivatives.

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

Nogawa, Hisashi published the artcilePharmacological characterisation of electrocardiogram J-T_peak interval in conscious Guinea pigs, Product Details of C17H18N2O6, the publication is European Journal of Pharmacology (2022), 175065, database is CAplus and MEDLINE.

Drug-induced human ether-a-́go-go-related gene (hERG) channel block and QT interval prolongation increase torsade de pointes (TdP) risk. However, some drugs block hERG channels and prolong QT interval with low TdP risk, likely because they block addnl. inward currents. We investigated the utility of J-T_peak interval, a novel biomarker of inward current block and TdP risk, in conscious telemetered guinea pigs. ECG parameters were analyzed in Hartley guinea pigs orally administered one of eight test compounds (dofetilide, flecainide, nifedipine, quinidine, quinine, ranolazine, sotalol, verapamil) or vehicle alone as controls. Heart rate-corrected QT (QTcX) and J-T_peak (J-T_peakcX) were calculated to evaluate the relations of QT-RR and J-T_peak-RR. Dofetilide and sotalol significantly increased ΔQTcX and ΔJ-T_peakcX intervals to similar degrees. Quinidine, quinine and flecainide also increased ΔQTcX and ΔJ-T_peakcX intervals, but the degrees of ΔJ-T_peakcX interval prolongation were shorter than those of ΔQTcX interval prolongation. Ranolazine showed slight increasing trends in ΔQTcX and ΔJ-T_peakcX intervals, but the differences were not significant. Verapamil and nifedipine did not increase the ΔQTcX or ΔJ-T_peakcX intervals. Based on the relations of ΔΔJ-T_peakcX and ΔΔQTcX intervals, dofetilide, sotalol and quinidine were classified as high risk for TdP, quinine, flecainide and ranolazine were classified as intermediate risk and verapamil and nifedipine were classified as low risk. These results supported the usefulness of J-T_peak interval assessment in conscious guinea pigs for predicting drug-induced balanced block of inward currents and TdP risk in early-stage preclin. studies.

European Journal of Pharmacology 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

Kamata, Ryo published the artcileAgonistic effects of diverse xenobiotics on the constitutive androstane receptor as detected in a recombinant yeast-cell assay, Computed Properties of 971-66-4, the publication is Toxicology In Vitro (2018), 335-349, database is CAplus and MEDLINE.

The constitutive androstane receptor (CAR) is a nuclear receptor and transcription factor regulating proteins involved in xenobiotic metabolism Agonist activation of the CAR can trigger metabolic activation and toxification as well as detoxification and clearance; accordingly, xenobiotic substances acting as CAR ligands may pose a threat to human and animal health. The authors used yeast cells transduced with the human CAR and the response pathway to measure the CAR-agonistic activities of 549 synthetic or natural compounds: 216 of the tested compounds exhibited CAR-agonistic effects. Eighty-four percent of CAR-activating compounds were aromatic compounds, and >65% of these active compounds were aromatic hydrocarbons, bisphenols, monoalkyl phenols, phthalates, styrene dimers, di-Ph ethers, organochlorines, and organophosphates. The ten most potent compounds were 4-tert-octylphenol (4tOP; reference substance), 4-nonylphenol, diethylstilbestrol, benzyl Bu phthalate, 2-(4-hydroxyphenyl)-2,4,4-trimethylchroman, o,p’-DDT, methoxychlor, di-Pr phthalate, hexestrol, and octachlorostyrene. The activities of these nine non-reference compounds exceeded 10% of the 4tOP activity. Anal. of para-monoalkyl phenols suggests that branching of the alkyl group and chlorination at the ortho position raises potency. This study provides critical information for identifying the potential of CAR-mediated toxic hazards and for understanding the relevant mechanism.

Toxicology In Vitro published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Computed Properties of 971-66-4.

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

Kucharski, Dawid published the artcileThe assessment of environmental risk related to the occurrence of pharmaceuticals in bottom sediments of the Odra River estuary (SW Baltic Sea), Quality Control of 21829-25-4, the publication is Science of the Total Environment (2022), 154446, database is CAplus and MEDLINE.

The occurrence of 130 pharmaceutically active compounds (PhACs) in sediments collected from 70 sampling sites in the Odra River estuary (SW Baltic Sea) was investigated. The highest concentration levels of the compounds were found in the vicinity of effluent discharge from two main Szczecin wastewater treatment plants: “Pomorzany” and “Zdroje”, and nearby the seaport and shipyard. The highest environmental risks (RQ > 1) were observed for pseudoephedrine (RQ = 14.0), clindamycin (RQ = 7.3), nalidixic acid (RQ = 3.8), carbamazepine (RQ = 1.8), fexofenadine (RQ = 1.4), propranolol (RQ = 1.1), and thiabendazole (RQ = 1.1). RQ for each compound varied depending on the sampling sites. High environmental risk was observed in 30 sampling sites for clindamycin, 22 sampling sites for pseudoephedrine, 19 sampling sites for nalidixic acid, 4 sampling sites for carbamazepine, and 3 sampling sites for fexofenadine. The medium environmental risk (0.1 < RQ < 1) was observed for 16 compounds: amisulpride, amitriptyline, amlodipine, atropine, bisoprolol, chlorpromazine, lincomycin, metoprolol, mirtazapine, moclobemide, ofloxacin, oxazepam, tiapride, tolperisone, verapamil, and xylometazoline. Due to the scarcity of toxicol. data related to benthic organisms, only an approx. assessment of the environmental risk of PhACs is possible. Nevertheless, the compounds with medium and high risk should be considered as pollutants of high environmental concern whose occurrence in the environment should remain under close scrutiny.

Science of the Total Environment 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, Quality Control of 21829-25-4.

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

Karunanithi, Srividhya published the artcileTocilizumab and Renal Artery Stent-Therapeutic Strategy for Takayasu Arteritis, Synthetic Route of 21829-25-4, the publication is Journal of Clinical Rheumatology and Immunology (2022), 22(1), 37-40, database is CAplus.

Takayasu vasculitis (TAK) is a form of large vessel vasculitis clin. manifesting as pulseless disease or hypertension. It is more common in South East Asia and Japan, India, and Mexico [1]. It is increasingly being recognized due to increased awareness among medical fraternity and better imaging modalities. Undetected hypertension, pulselessness, and syncope are more common symptoms and presentation during pregnancy is unusual and can lead to bad obstetric outcomes. Recent evidences support the use of tocilizumab for inducing remission in Takayasu arteritis. We report this rare case of vasculitis presenting in pregnancy as malignant hypertension. A 20-yr-old pregnant woman (45 days) presented with headache and nausea but no fever. She had a history of intermittent claudication of legs for the past 3 years but not evaluated. During examination, pulses were felt normally and blood pressure (BP) 180/110, no murmurs in cardiac auscultation, but she had abdominal bruit (renal vessels). Other systems were normal. Echocardiogram (ECHO) showed dilated ascending aorta. Doppler of renal vessels showed narrowing of renal arteries. Unfortunately, she had to undergo termination of pregnancy (high BP in spite of antihypertensives). Her computed tomog. (CT) angiogram showed features of TAK with type 5 pattern-she had methylprednisolone infusion 500 mg daily for 3 days, followed by injection tocilizumab 400 mg monthly 3 doses. Once remission was achieved, she had recanalization by percutaneous transluminal angioplasty of right renal artery. She is currently maintained on aspirin and telmisartan. Awareness of causes of high BP, inputs by radiologist, cardiologist, and rheumatologist and understanding by the patient and family helped to achieve good outcome albeit the miscarriage.

Journal of Clinical Rheumatology and Immunology 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

Ishida, Naoki published the artcileSynthesis of Amine-Borane Intramolecular Complexes through Palladium-Catalyzed Rearrangement of Ammonioalkynyltriarylborates, Recommanded Product: Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Organic Letters (2008), 10(6), 1279-1281, database is CAplus and MEDLINE.

The Pd-catalyzed rearrangement reaction of alkynyltriarylborates having a tertiary ammonium moiety stereoselectively afforded amine-borane intramol. complexes, some of which exhibited significantly strong fluorescence. E.g., under Ar atm. a mixture of Me₂N⁺HCH₂CCB^–Ph₃, 2.5 mol% Pd₂(dba)₃·CHCl₃/P(o-tol)₃ in THF was stirred at 70° to give 91% yield of cyclic dimethyl{(E)-3-phenyl-3-diphenylborylprop-2-enyl}amine.

Organic Letters published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Recommanded Product: Triphenyl(pyridin-1-ium-1-yl)borate.

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

Ishida, Naoki published the artcileStereoselective synthesis of trisubstituted alkenylboranes by palladium-catalysed reaction of alkynyltriarylborates with aryl halides, Name: Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Chemical Communications (Cambridge, United Kingdom) (2007), 4381-4383, database is CAplus and MEDLINE.

The palladium-catalyzed reaction of alkynyltriarylborates with aryl halides afforded trisubstituted alkenylboranes, in which two different aryl groups were installed across the carbon-carbon double bond in a cis arrangement.

Chemical Communications (Cambridge, United Kingdom) published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, Name: Triphenyl(pyridin-1-ium-1-yl)borate.

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

Hate, Siddhi S. published the artcileA Mechanistic Study of Drug Mass Transport from Supersaturated Solutions Across PAMPA Membranes, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) (2022), 111(1), 102-115, database is CAplus and MEDLINE.

There is an increasing shift from dissolution testing to dissolution-permeation testing of formulations during formulation development and this has led increasing application of permeability measurements using parallel artificial membrane permeability assay (PAMPA) membranes. However, there is a lack of thorough anal. of the impact of variabilities in the PAMPA setup on the mass flow rate outcomes, particularly for complex solubility-enabling formulations. In this study, we investigated the impact of amorphous drug-rich nanodroplets, formed in supersaturated solutions by liquid-liquid phase separation, on membrane transport by measuring mass flow rate across PAMPA membranes. In addition, we explored the impact of PAMPA variants such as lipid composition, hydrophobicity and pore size of the filter support, as well as receiver sink properties on membrane mass flow rates of solutions containing amorphous nanodroplets. Filter properties and lipid composition did not show a notable influence on the mass flow rates for lipophilic mols., while a marked impact was observed for hydrophilic mols. High sink conditions in the receiver compartment, arising from addition of micellar surfactant, altered the membrane integrity for lipid-impregnated hydrophilic membranes. In contrast, no such effect was observed for a hydrophobic filter support. Membrane integrity tests also suggested that monitoring water transport may be an improved approach over using Lucifer yellow. Furthermore, high sink conditions in the receiver compartment resulted in an increase in the overall mass flow rate. This was due to the effect of asym. conditions, generated across the membrane, on mass transport kinetics. Linearity between mass flow rate and donor concentration was observed until the donor concentration reached the amorphous solubility Above the amorphous solubility, a gradual increase in mass flow rate was observed i.e., with an increasing number of nanodroplets in the solution This was attributed to decrease in the permeability barrier across unstirred water layer due to reduction of the concentration gradient as nanodroplets dissolved to replenish absorbed drug. Observations made in this study provide insights into the mechanisms associated with mass transport of supersaturated solutions across PAMPA membranes, which are critical for improved evaluation of enabling formulations.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) 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, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Hartung, Jane E. published the artcileVoltage-gated calcium currents in human dorsal root ganglion neurons, Quality Control of 21829-25-4, the publication is Pain (2022), 163(6), e774-e785, database is CAplus and MEDLINE.

Voltage-gated calcium channels in sensory neurons underlie processes ranging from neurotransmitter release to gene expression and remain a therapeutic target for the treatment of pain. Yet virtually all we know about voltage-gated calcium channels has been obtained through the study of rodent sensory neurons and heterologously expressed channels. To address this, high voltage-activated (HVA) Ca²⁺ currents in dissociated human and rat dorsal root ganglion neurons were characterized with whole-cell patch clamp techniques. The HVA currents from both species shared basic biophys. and pharmacol. properties. However, HVA currents in human neurons differed from those in the rat in at least 3 potentially important ways: (1) Ca²⁺ c.d. was significantly smaller, (2) the proportion of nifedipine-sensitive currents was far greater, and (3) a subpopulation of human neurons displayed relatively large constitutive current inhibition. These results highlight the need to for the study of native proteins in their native environment before initiating costly clin. trials.

Pain 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, Quality Control of 21829-25-4.

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

Santana-Mateos, Marta published the artcileClinical and Pharmacological Parameters Determine Relapse During Clopidogrel Treatment of Acute Coronary Syndrome, Product Details of C17H18N2O6, the publication is Journal of Clinical Pharmacology (2022), 62(6), 783-791, database is CAplus and MEDLINE.

The therapeutic efficacy of clopidogrel as an antiplatelet drug varies among individuals, being the mainstream hypothesis that its bioavailability depends on the individual genetic background and/or interactions with other drugs. A total of 477 patients receiving double antiaggregation therapy with aspirin and clopidogrel, after suffering a first event, were followed for 1 yr to record relapse, as a surrogate end point to measure their therapeutic response, as defined by presenting with an acute coronary event (unstable angina, ST-segment-elevation myocardial infarction, or non-ST-segment-elevation myocardial infarction), stent thrombosis/restenosis, or cardiac mortality. Anthropometric, clin., and pharmacol. variables along with CYP2C19 genotypes were analyzed for their association with the disease relapse phenotype. Only 75 patients (15%) suffered a relapse, which occurred during the first 6 mo of therapy, with a peak at 4.5 mo. An initial univariate anal. identified that patients in the relapse group were significantly older (67.4 ± 11.0 vs 61.6 ± 12.3 years old) and presented with diffuse coronary disease, insulin-dependent type 2 diabetes mellitus dyslipidemia, and arterial hypertension. A poor clin. response to the platelet antiaggregation regime also occurred more frequently among patients taking acenocoumarol and calcium channel blockers, along with aspirin and clopidogrel, while no association was found according to CYP2C19 genotypes. A retrospective multivariate anal. indicated that patients belonging to the nonresponder phenotype to treatment with aspirin and clopidogrel were older, presented with diffuse coronary disease, a group largely overlapping with type 2 insulin-dependent diabetes mellitus, and were taking dihidropyrimidinic calcium channel blockers.

Journal of Clinical Pharmacology 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