Tag: M.W=300-350

Saraf, Isha published the artcileForced Solid-State Oxidation Studies of Nifedipine-PVP Amorphous Solid Dispersion, Computed Properties of 21829-25-4, the publication is Molecular Pharmaceutics (2022), 19(2), 568-583, database is CAplus and MEDLINE.

In the present study, the oxidative degradation behavior of nifedipine (NIF) in amorphous solid dispersions (ASDs) prepared with poly(vinyl pyrrolidone) (PVP) with a short (K30) and a long (K90) chain length was investigated. The ASDs were prepared via dry ball-milling and analyzed using Fourier transform IR (IR) spectroscopy, X-ray scattering, and differential scanning calorimetry. The ASDs were exposed to accelerated thermal-oxidative conditions using a pressurized oxygen headspace (120 °C for 1 day) and high temperatures at atm. pressure (60-120 °C for a period of 42 days). Addnl., solution-state oxidative degradation studies showed that pure NIF degrades to a greater extent than in the presence of PVP. Electronic structure calculations were performed to understand the impact of drug-polymer intermol. interactions on the autoxidation of drugs. While no drug degradation was observed in freshly prepared ASD samples, alkyl free radicals were detected via ESR (EPR) spectroscopy. The free radicals were found to be consumed to a greater extent by PVP K30- than PVP K90-based ASDs upon exposure to high oxygen pressures. This was consistent with the greater solid-state oxidative degradation of NIF observed in ASDs with PVP K30 than with PVP K90. As no drug recrystallization occurred during this study period, the lower glass-transition temperature and presumed greater mol. mobility of PVP K30 and its ASD as compared to the PVP K90 system appear to contribute to the greater drug degradation in PVP-K30-based ASDs. The extent and the rate of oxidative degradation were higher in the case of PVP-K30-based ASD as compared to that in PVP-K90-based ASD, and the overall degradation increased with an increase in temperature IR spectral anal. of drug-polymer interactions supports the electronic calculations of the oxidation process. We infer that, apart from the initial free radical content, the difference in the extent of drug-polymer intermol. interactions in ASDs and amorphous stabilization during the forced oxidation experiments contribute to the observed differences in the autoxidative reactivity of the drug in ASDs with different PVP chain lengths. Overall, the chem. degradation of NIF in ASDs with two PVP chain lengths obtained from accelerated solid-state oxidation studies was in qual. agreement with that obtained from long-term (3 years) storage under ambient conditions. The study highlights the ability of accelerated processes to determine the oxidative degradation behavior of polymeric ASDs and suggests that the polymer chain length could factor into chem. as well as phys. stability considerations.

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 C17H18N2O6, Computed Properties of 21829-25-4.

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

Sarkar, Abhijit published the artcileDendritic polymer networks: a new class of nano-domained environmentally benign antifouling coatings, Category: pyridine-derivatives, the publication is ACS Symposium Series (2009), 165-186, database is CAplus.

A new type of antifouling coatings for application in both fresh water and marine environments has been developed utilizing dendritic polymer nanotechnol. The resulting coatings are capable of encapsulating and strongly binding electrophilic biocides in their dendritic nano-cells, where biocides retain their antifouling activity while being prevented from leaching and polluting the aquatic environment. These coatings for the first time successfully combine the best properties of non-stick and biocide-containing coatings and provide an environment-ally benign solution for the protection of man-made objects.

ACS Symposium Series 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, Category: pyridine-derivatives.

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

Ravasenga, Tiziana published the artcileSpatial regulation of coordinated excitatory and inhibitory synaptic plasticity at dendritic synapses, SDS of cas: 21829-25-4, the publication is Cell Reports (2022), 38(6), 110347, database is CAplus and MEDLINE.

The induction of synaptic plasticity at an individual dendritic glutamatergic spine can affect neighboring spines. This local modulation generates dendritic plasticity microdomains believed to expand the neuronal computational capacity. Here, we investigate whether local modulation of plasticity can also occur between glutamatergic synapses and adjacent GABAergic synapses. We find that the induction of long-term potentiation at an individual glutamatergic spine causes the depression of nearby GABAergic inhibitory synapses (within 3 μm), whereas more distant ones are potentiated. Notably, L-type calcium channels and calpain are required for this plasticity spreading. Overall, our data support a model whereby input-specific glutamatergic postsynaptic potentiation induces a spatially regulated rearrangement of inhibitory synaptic strength in the surrounding area through short-range heterosynaptic interactions. Such local coordination of excitatory and inhibitory synaptic plasticity is expected to influence dendritic information processing and integration.

Cell Reports 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, SDS of cas: 21829-25-4.

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

Feiteiro, Joana published the artcilePathways involved in the human vascular Tetrabromobisphenol A response: Calcium and potassium channels and nitric oxide donors, Category: pyridine-derivatives, the publication is Toxicology (2022), 153158, database is CAplus and MEDLINE.

Tetrabromobisphenol A (TBBPA) is a flame retardant that can contaminate the environment and human being, acting as an endocrine disruptor. Several studies propose a correlation between TBBPA exposure and adverse health outcomes, however, at vascular level TBBPA effects are still poorly understood. Thus, considering that the vascular tonus is regulated by vasoactive substances (serotonin and histamine) which are involved in some pathol. processes, this work aimed to analyze the direct effects and the 24 h exposure of TBBPA on the human umbilical artery (HUA) and to investigate its signalling pathway. Using organ bath technique, endothelium-denuded HUA rings were contracted with serotonin (5-HT, 1 μM), histamine (His, 10 μM) and potassium chloride (KCl, 60 mM), and the exposure (0-24 h) of different concentrations of TBBPA (1, 10 and 50 μM) were evaluated. Besides, the vascular mode of action of TBBPA was studied through the anal. of cyclic guanosine monophosphate and calcium channels activity, pathways involved in relaxation and contraction of HUA, resp. Our results demonstrated that the direct effects of TBBPA induce a vasorelaxation of HUA. The maximum relaxant effect was observed at 100 μM of TBBPA with 63.74%, 64.24% and 30.05%, for 5-HT-, His- or KCl-contracted arteries resp. The 24 h TBBPA exposure altered the vasorelaxant response pattern of sodium nitroprusside and nifedipine. This effect is due to the involvement of TBBPA with the NO/sGC/cGMP/PKG pathway and the interference in calcium influx. Furthermore, using the real-time quant. polymerase chain reaction, TBBPA clearly modulates -type calcium and large-conductance Ca2+ 1.1 α- and β1 -subunit channels, and soluble guanylyl cyclase and protein Kinase G. So, at vascular level TBBPA induces changes in HUA after TBBPA exposure.

Toxicology 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, Category: pyridine-derivatives.

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

Galuashvili, Zh. S. published the artcileEnergy of triphenylboron pπ-conjugation, Product Details of C23H20BN, the publication is Doklady Akademii Nauk SSSR (1972), 207(1), 99-101 [Chem], database is CAplus.

Heats of formation of complexes of Ph3B with pyridine (I) and 4-methylpyridine and of Et3B with I, and their dipole moments in C6H6 and dioxane were determined and used to evaluate pπ-resonance in Ph3B. The low value of pπ-resonance in Ph3B is about an order of magnitude smaller than that of π-bonding, calling for care in the use of quantum-mechanics calculations in estimation of rearrangement energies in electron acceptor mols. The degree of charge transfer in these complexes was 0.45 for those of Ph3B and 0.34 for Et3B-I.

Doklady Akademii Nauk SSSR 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, Product Details of C23H20BN.

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

Gunaratne, Gihan S. published the artcileIdentification of a dihydropyridine scaffold that blocks ryanodine receptors, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is iScience (2022), 25(1), 103706, database is CAplus and MEDLINE.

Ryanodine receptors (RyRs) are large, intracellular ion channels that control Ca²⁺ release from the sarco/endoplasmic reticulum. Dysregulation of RyRs in skeletal muscle, heart, and brain has been implicated in various muscle pathologies, arrhythmia, heart failure, and Alzheimer′s disease. Therefore, there is considerable interest in therapeutically targeting RyRs to normalize Ca²⁺ homeostasis in scenarios involving RyR dysfunction. Here, a simple invertebrate screening platform was used to discover new chemotypes targeting RyRs. The approach measured Ca²⁺ signals evoked by cyclic ADP ribose, a second messenger that sensitizes RyRs. From a 1,534-compound screen, FLI-06 (currently described as a Notch “inhibitor”) was identified as a potent blocker of RyR activity. Two closely related tyrosine kinase inhibitors that stimulate and inhibit Ca²⁺ release through RyRs were also resolved. Therefore, this simple screen yielded RyR scaffolds tractable for development and revealed an unexpected linkage between RyRs and trafficking events in the early secretory pathway.

iScience 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Novais, Teddy published the artcilePotentially inappropriate medications and anticholinergic and sedative burden in older patients with haemophilia or von Willebrand disease: The M’HEMORRH-AGE study, Category: pyridine-derivatives, the publication is Journal of Clinical Pharmacy and Therapeutics (2022), 47(6), 783-791, database is CAplus and MEDLINE.

In older patients, multiple chronic conditions lead to the intake of multiple medications and a higher risk of adverse drug events. The exposure to inappropriate medications in older patients with bleeding disorders is poorly explored. The aim of this study was to describe the exposure to potentially inappropriate medications (PIMs) and medications with anticholinergic and sedative properties in older community-dwelling patients with haemophilia or von Willebrand Disease (VWD). The M’HEMORRH-AGE study (Medication in AGEd patients with HAEMORRHagic disease) is a multicentre prospective observational study. Community-dwelling patients over 65 years with haemophilia or VWD were included in the study. PIMs were identified using the EU(7)-PIM list, and the anticholinergic and sedative drug exposure was measured using the Drug Burden Index. In 142 older community-dwelling patients with haemophilia (n = 89) or VWD (n = 53) were included (mean age: 72.8 ± 5.8 years). PIMs were used by 45.8% of older patients and were mainly represented by cardiovascular (34.9%), nervous systems (26.7%) and alimentary tract and metabolism PIMs (25.6%). Regarding anticholinergic and/or sedative medications, 37.3% of older patients were exposed mainly due to nervous system medications (68.3%), for example analgesics. The MHEMORRH-AGE study showed the exposure to PIMs and anticholinergic/sedative medications was high in older community-dwelling patients with haemophilia or VWD. Interventions focusing on deprescription of these inappropriate medications should be conducted in this specific population.

Journal of Clinical Pharmacy and Therapeutics 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, Category: pyridine-derivatives.

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

Greenwood, Norman N. published the artcileProperties and thermochemistry of complexes of pyridine with triphenyl-boron, -aluminum, -gallium, and -indium, and diphenylgallium chloride, Recommanded Product: Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Journal of the Chemical Society [Section] A: Inorganic, Physical, Theoretical (1969), 249-53, database is CAplus.

Pyridine reacts with crystalline Ph3B, Ph3Al, Ph3Ga, Ph3In, and Ph2GaCl to give white 1:1 complexes which are monomeric in benzene solution The melting points and heats of formation of the solid adducts from liquid pyridine and crystalline acceptors are: Ph3B. py, 240°, 17.9 kcal. mole-1; Ph3Al.py, 168°, 22.3 kcal. mole-1; Ph3Ga.py, 167°, 19.5 kcal. mole-1; Ph3In.py, 130°, 13.9 kcal. mole-1; Ph2GaCl.py, 18.0 kcal. mole.-1 The problems attending the estimation of gas-phase heats of formation and the calculation of reorganization energies are discussed and the results compared with those available on other Group III acceptors.

Journal of the Chemical Society [Section] A: Inorganic, Physical, Theoretical 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

Fernandez, M. A. published the artcileNew approaches for monitoring the marine environment: the case of antifouling paints, Related Products of pyridine-derivatives, the publication is International Journal of Environment and Health (2007), 1(3), 427-448, database is CAplus.

A review. Protection of ships hulls against biofouling has been a problem since man began sailing the seas. The most common protections are specially produced antifouling paints. These paints could be broadly classified in three main groups, or generations, depending on the technol. applied: first generation copper-based, second generation organotin-based, and the new, third generation, organotin-free antifouling paints. Most of these new paints contain biocides, and consequently are also toxic. To further complicate risk evaluations, synergistic effects occurred when mixtures were tested. Some researchers have pointed out the risk of employing these compounds without a deep knowledge of their environmental behavior and their effects on marine communities. However, the transition from second to third generation antifoulings is now a reality. Therefore, in this paper, considerations on the chem. and ecotoxicol. information required and proposals for approaches to deal with the new antifouling problems are discussed.

International Journal of Environment and Health 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, Related Products of pyridine-derivatives.

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

Macedo, Cicero Andre Ferreira published the artcileLippia origanoides essential oil induces tocolytic effect in virgin rat uterus and inhibits writhing in a dysmenorrhea mouse model, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Ethnopharmacology (2022), 115099, database is CAplus and MEDLINE.

The species Lippia origanoides Kunth, popularly known as “salva-de-marajo”, is used in Brazilian traditional “quilombola” communities to treat menstrual cramps and uterine inflammation. Evaluate the spasmolytic activity of Lippia origanoides essential oil (LOO) on exptl. models of uterine conditions related to menstrual cramps and investigate its mechanism of action. Virgin rat-isolated uterus was mounted in the organ bath apparatus to evaluate the spasmolytic effect of LOO on basal tonus and contractions induced by carbachol, KCl, or oxytocin. We used pharmacol. agents to verify the relaxation mechanism of LOO. The evaluation of uterine contractility in virgin rats, after treatment with LOO for three consecutive days, was carried out by the construction of a concentration-response curve with oxytocin or carbachol. The primary dysmenorrhea animal model was replicated with an injection of estradiol cypionate in female mice for three consecutive days, followed by i.p. application of oxytocin. LOO relaxed the rat uterus precontracted with 10-2 IU/mL oxytocin (logEC50 = 1.98 ± 0.07), 1μM carbachol (logEC50 = 1.42 ± 0.07) or 60 mM KCl (logEC50 = 1.53 ± 0.05). It was also able relax uterus on spontaneous contractions (logEC50 = 0.41 ± 0.05). Preincubation with glibenclamide, propranolol, phentolamine or L-NAME in contractions induced by carbachol did not alter significantly the relaxing effect of LOO. However, in the presence of 4-aminopyridine, CsCl or tetraethylammonium there was a reduction of LOO potency, whereas the blockers methylene blue, ODQ, aminophylline and heparin potentiated the LOO relaxing effect. Preincubation with LOO in a Ca2+ free medium at concentrations of 27μg/mL or 81μg/mL reduced the contraction induced by carbachol. The administration of LOO for 3 days did not alter uterus contractility. The treatment with LOO at 30 or 100 mg/kg i.p., or 100 mg/kg orally, inhibited writhing in female mice. The association of LOO at 10 mg/kg with nifedipine or mefenamic acid potentiated writhing inhibition in mice.The essential oil of L. origanoides has tocolytic activity in rat isolated uterus pre-contracted with KCl, oxytocin, or carbachol. This effect is possibly related to the opening of potassium channels (Kir, KV, and KCa), cAMP increase, and diminution of intracellular Ca2+. This relaxant effect, probably, contributed to reduce the number of writhings in an animal model of dysmenorrhea being potentiated by nifedipine or mefenamic acid. Taken together, the results here presented indicate that this species has a pharmacol. potential for the treatment of primary dysmenorrhea, supporting its use in folk medicine.

Journal of Ethnopharmacology 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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