Day: December 21, 2022

Souza de Araujo, Guilherme Rodolfo published the artcileMicroemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: Structural and in vitro study, SDS of cas: 21829-25-4, the main research area is PPG5CETETH20 nifedipine microemulsion transdermal delivery skin permeation; Drug Delivery System(s); Microemulsion(s); Nanotechnology; Surfactant(s); Transdermal.

Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility This study aimed to develop a microemulsified system with low surfactant concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index < 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers, acting by rising the coefficients of partition and diffusion of the nifedipine in the skin. Colloids and Surfaces, B: Biointerfaces published new progress about Anisotropy. 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

Gierten, Jakob published the artcileAutomated high-throughput heartbeat quantification in medaka and zebrafish embryos under physiological conditions, Related Products of pyridine-derivatives, the main research area is nifedipine cardioprotectant embryo heartbeat Oryzias Danio cardiovascular development.

Abstract: Accurate quantification of heartbeats in fish models is an important readout to study cardiovascular biol., disease states and pharmacol. However, dependence on anesthesia, laborious sample orientation or requirement for fluorescent reporters have hampered the use of high-throughput heartbeat anal. To overcome these limitations, we established an efficient screening assay employing automated label-free heart rate determination of randomly oriented, non-anesthetized medaka (Oryzias latipes) and zebrafish (Danio rerio) embryos in microtiter plates. Automatically acquired bright-field data feeds into an easy-to-use HeartBeat software with graphical user interface for automated quantification of heart rate and rhythm. Sensitivity of the assay was demonstrated by profiling heart rates during entire embryonic development. Our anal. revealed rapid adaptation of heart rates to temperature changes, which has implications for standardization of exptl. layout. The assay allows scoring of multiple embryos per well enabling a throughput of >500 embryos per 96-well plate. In a proof of principle screen for compound testing, we captured concentration-dependent effects of nifedipine and terfenadine over time. Our novel assay permits large-scale applications ranging from phenotypic screening, interrogation of gene functions to cardiovascular drug development.

Scientific Reports published new progress about Anesthesia. 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bischoff, Angela published the artcileEffects of Nifedipine on Renal and Cardiovascular Responses to Neuropeptide Y in Anesthetized Rats, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is nifedipine renal cardiovascular response neuropeptide Y anesthesia; Y1 receptor; Y5 receptor; blood pressure; diuresis; natriuresis; neuropeptide Y; nifedipine; renal blood flow.

Neuropeptide Y (NPY) acts via multiple receptor subtypes termed Y1, Y2 and Y5. While Y1 receptor-mediated effects, e.g., in the vasculature, are often sensitive to inhibitors of L-type Ca2+ channels such as nifedipine, little is known about the role of such channels in Y5-mediated effects such as diuresis and natriuresis. Therefore, we explored whether nifedipine affects NPY-induced diuresis and natriuresis. After pre-treatment with nifedipine or vehicle, anesthetized rats received infusions or bolus injections of NPY. Infusion NPY (1μg/kg/min) increased diuresis and natriuresis, and this was attenuated by i.p. injection of nifedipine (3μg/kg). Concomitant decreases in heart rate and reductions of renal blood flow were not attenuated by nifedipine. Bolus injections of NPY (0.3, 1, 3, 10 and 30μg/kg) dose-dependently increased mean arterial pressure and renovascular vascular resistance; only the higher dose of nifedipine (100μg/kg/min i.v.) moderately inhibited these effects. We conclude that Y5-mediated diuresis and natriuresis are more sensitive to inhibition by nifedipine than Y1-mediated renovascular effects. Whether this reflects a general sensitivity of Y5 receptor-mediated responses or is specific for diuresis and natriuresis remains to be investigated.

Molecules published new progress about Anesthesia. 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, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chen, Jinqin published the artcileA novel ω-conotoxin Bu8 inhibiting N-type voltage-gated calcium channels displays potent analgesic activity, HPLC of Formula: 21829-25-4, the main research area is conotoxin voltage gated calcium channel analgesic activity; Analgesic activity; Bu8; DIEA, diisopropylethylamine; ESI-MS, electrospray ionization-mass spectroscopy; Fmoc, N-(9-fluorenyl)methyloxy-carbonyl; HBTU, 2-(1H-benzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; HOBt, 1-hydroxybenzotriazole; IC50, half-maximal inhibitory concentration; N-type calcium ion channel; RP-HPLC, reversed phase high-performance liquid chromatography; Structure–activity relationship; TFA, trifluoroacetic acid; ω-conotoxin.

A ω-Conotoxins inhibit N-type voltage-gated calcium (CaV2.2) channels and exhibit efficacy in attenuating neuropathic pain but have a low therapeutic index. Here, we synthesized and characterized a novel ω-conotoxin, Bu8 from Conus bullatus, which consists of 25 amino acid residues and three disulfide bridges. Bu8 selectively and potently inhibits depolarization-activated Ba2+ currents mediated by rat CaV2.2 expressed in HEK293T cells (IC50 = 89 nmol/L). Bu8 is two-fold more potent than ω-conotoxin MVIIA, a ω-conotoxin currently used for the treatment of severe chronic pain. It also displays potent analgesic activity in animal pain models of hot plate and acetic acid writhing but has fewer side effects on mouse motor function and lower toxicity in goldfish. Its lower side effects may be attributed to its faster binding rate and higher recovery ratios. The NMR structure demonstrates that Bu8 contains a small irregular triple β-strand. The structure-activity relationships of Bu8 Ala mutants and Bu8/MVIIA hybrid mutants demonstrate that the binding mode of CaV2.2 with the amino acid residues in loop 1 and loop 2 of Bu8 is different from that of MVIIA. This study characterizes a novel, more potent ω-conotoxin and provides new insights for designing CaV2.2 antagonists.

Acta Pharmaceutica Sinica B published new progress about Analgesics. 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

Swanson, Devin M. published the artcileIdentification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist, Computed Properties of 306934-70-3, the main research area is vanilloid receptor antagonist preparation analgesic.

High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified the essential pharmacophoric elements for antagonism that permitted further optimization via targeted synthesis to provide a potent orally bioavailable and selective TRPV1 modulator 41 active in several in vivo models.

Journal of Medicinal Chemistry published new progress about Analgesics. 306934-70-3 belongs to class pyridine-derivatives, name is 1-(5-(Trifluoromethyl)pyridin-2-yl)-1,4-diazepane, and the molecular formula is C11H14F3N3, Computed Properties of 306934-70-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Lamberto, Massimiliano published the artcileMicrowave-assisted synthesis of symmetric and asymmetric viologens, SDS of cas: 36437-30-6, the main research area is sym asym viologen microwave assisted synthesis.

Viologens are generally synthesized by N-alkylating 4,4′-bipyridine with alkyl halides. Under conventional heating conditions, however, their synthesis suffers from long reaction times and, often, low yields. In this work, sym. and asym. viologens were synthesized under the assistance of microwave irradiation in good to excellent yields and in short reaction times.

Tetrahedron Letters published new progress about Alkylation. 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, SDS of cas: 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Schmidt, Michael A. published the artcileEffect of Terminal Alkylation of Aryl and Heteroaryl Hydrazines in the Fischer Indole Synthesis, Computed Properties of 3469-63-4, the main research area is Fischer indole synthesis; hydrazine ketone alkylation amidation cross coupling.

The effect of alkylation on the terminal position of aryl and heteroaryl hydrazines in the Fischer indole synthesis was examined Compared to their unalkylated counterparts, reactions using alkylated s provided indole products with higher yields and faster rates. The reactions can be conducted at lower temperatures and are compatible with acid-sensitive functionality. The terminally alkylated hydrazines were readily prepared by a new two-step sequence and held as stable hydrazinium salts. The mild formation of the salts along with the favorable Fischer indole reaction conditions highlights the potential of this approach in later-stage synthetic use.

Journal of Organic Chemistry published new progress about Alkylation. 3469-63-4 belongs to class pyridine-derivatives, name is Ethyl 5-methoxy-1H-pyrrolo[2,3-c]pyridine-2-carboxylate, and the molecular formula is C11H12N2O3, Computed Properties of 3469-63-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Palmquist, Karl H. published the artcileReciprocal cell-ECM dynamics generate supracellular fluidity underlying spontaneous follicle patterning, Quality Control of 21829-25-4, the main research area is supracellular fluidity extracellular matrix follicle cell; active soft matter; biophysics; contractility; emergence; extracellular matrix; mechanics; mechanosensation; morphogenesis; multicellular; organogenesis; periodic patterning; self-organization; skin.

During vertebrate embryogenesis, cell collectives engage in coordinated behavior to form tissue structures of increasing complexity. In the avian skin, assembly into follicles depends on intrinsic mech. forces of the dermis, but how cell mechanics initiate pattern formation is not known. Here, we reconstitute the initiation of follicle patterning ex vivo using only freshly dissociated avian dermal cells and collagen. We find that contractile cells phys. rearrange the extracellular matrix (ECM) and that ECM rearrangement further aligns cells. This exchange transforms a mech. unlinked collective of dermal cells into a continuum, with coherent, long-range order. Combining theory with experiment, we show that this ordered cell-ECM layer behaves as an active contractile fluid that spontaneously forms regular patterns. Our study illustrates a role for mesenchymal dynamics in generating cell-level ordering and tissue-level patterning through a fluid instability-processes that may be at play across morphol. symmetry-breaking contexts.

Cell (Cambridge, MA, United States) published new progress about Aggregates. 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

Zadymova, N. M. published the artcileAdsorption of a Lipophilic Drug, Felodipine, at Different Interfaces, COA of Formula: C18H19Cl2NO4, the main research area is adsorption lipophilic drug felodipine different interface.

In connection with the development of methods for the delivery of lipophilic drugs in a bioavailable form, we have employed an integrated approach to the investigation of the adsorption of an antihypertensive drug, felodipine, at interfaces that simulate the surfaces of different carriers. Isotherms have been plotted for felodipine adsorption from solutions in heptane (C = 2.13 x 10-5 – 4.26 x 10-4 M) at interfaces with water and silver metal, as well as for the compression of drug monolayers formed on a water surface from the heptane solutions The quant. characteristics of the studied felodipine layers have been determined, and their phase state and the most probable conformation of adsorbed drug mols. have been analyzed taking into account the data of mol. dynamics simulations. The phase state of the felodipine layers at the heptane/water interface is adequately described by the van Laar equation. A bilayer is formed at the silver surface. A phase transition from a gaseous state to a liquid-expanded state has been revealed for the felodipine layers.

Colloid Journal published new progress about Adsorption. 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, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mayer, Joachim M. published the artcileDeviations in the log P (partition coefficient) of protonated arylalkylamines and in their apparent log P, COA of Formula: C7H11ClN2, the main research area is amine aryl protonated partition coefficient; pyridylamine partition coefficient; phenylalkylamine partition coefficient.

Partition coefficients of monoprotonated phenyl- and 2-, 3-, and 4-pyridyl-substituted alkylamines show unpredictable but consistent trends. The coefficients of the Me, Bu, and pentyl homologs in each series are linearly related, while the Et and Pr derivatives appear too lipophilic. Thus, these partition coefficients are affected by perturbative effects, e.g., hydration or ion pairing. Also, the phosphate buffers yield abnormally low partition coefficient values.

European Journal of Medicinal Chemistry published new progress about Additivity. 84359-16-0 belongs to class pyridine-derivatives, name is 2-(Pyridin-3-yl)ethanamine hydrochloride, and the molecular formula is C7H11ClN2, COA of Formula: C7H11ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem