Month: December 2022

Motomura, Naoki published the artcileVisualization of calcium channel blockers in human adrenal tissues and their possible effects on steroidogenesis in the patients with primary aldosteronism (PA), Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Steroid Biochemistry and Molecular Biology (2022), 106062, database is CAplus and MEDLINE.

Voltage-gated L-type calcium channel (CaV) isoforms are well known to play pivotal tissue-specific roles not only in vasoconstriction but also in adrenocortical steroidogenesis including aldosterone biosynthesis. Alpha-1C subunit calcium channel (CC) (CaV1.2) is the specific target of anti-hypertensive CC blockers (CCBs) and its Alpha-1D subunit (CaV1.3) regulates depolarization of cell membrane in aldosterone-producing cells. Direct effects of CCBs on aldosterone biosynthesis were previously postulated but their intra-adrenal distribution and effects on steroid production in primary aldosteronism (PA) patients have remained virtually unknown. In this study, frozen tissue specimens constituting tumor, adjacent adrenal gland and peri-adrenal adipose tissues of nine aldosterone-producing adenoma (APA) cases were examined for visualization of amlodipine and aldosterone themselves using matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI). Liquid chromatog.-mass spectrometry (LC-MS) anal. was also performed to quantify amlodipine and 17 adrenal steroids in those cases above and compared the findings with immunohistochem. anal. of steroidogenic enzymes and calcium channels (CaV1.2 and CaV1.3). Effects of amlodipine on mRNA level of aldosterone biosynthetic enzymes were also explored using human adrenocortical carcinoma cell line (H295R). Amlodipine-specific peak (m/z 407.1 > 318.1) was detected only in amlodipine treated cases. Accumulation of amlodipine was marked in adrenal cortex compared to peri-adrenal adipose tissues but not significantly different between APA tumors and adjacent adrenal glands, which was subsequently confirmed by LC-MS quantification. Intra-adrenal distribution of amlodipine was generally consistent with that of CCs. In addition, quant. steroid profiles using LC-MS and in vitro study demonstrated the lower HSD3B activities in amlodipine treated cases. Immunoreactivity of CaV1.2 and HSD3B2 were also correlated. We report the first demonstration of specific visualization of amlodipine in human adrenal tissues by MALDI-MSI. Marked amlodipine accumulation in the adrenal glands suggested its direct effects on steroidogenesis in PA patients, possibly targeting on CaV1.2 and suppressing HSD3B activity.

Journal of Steroid Biochemistry and Molecular Biology 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

Kawasaki-Takasuka, Tomoko published the artcileThe modified trifluoromethylation protocol applicable to electronically deficient iodopyridinones, Computed Properties of 197958-29-5, the publication is Tetrahedron (2015), 71(38), 6824-6831, database is CAplus.

Utilization of a mixed solvent system of DMF/HMPA = 1/1 (volume/volume) to the KF/CuI/TMSCF₃ reagent system proved to significantly affect the reaction, realizing convenient introduction of a trifluoromethyl (CF₃) group not only to electron-deficient iodopyridinones, e.g., I, with quite a few previous successful examples but also to aliphatic vinylic iodides such as 2-iodocyclohex-2-en-1-one, 1-iodocyclohex-1-ene, (E)- and (Z)-(4-iodobut-3-en-1-yl)benzene.

Tetrahedron published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Computed Properties of 197958-29-5.

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

Tanaka, Ryo published the artcileCatalytic Hydrogenation of Carbon Dioxide Using Ir(III)-Pincer Complexes, Recommanded Product: 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, the publication is Journal of the American Chemical Society (2009), 131(40), 14168-14169, database is CAplus and MEDLINE.

Catalytic hydrogenation of carbon dioxide in aqueous potassium hydroxide was performed using a newly synthesized isopropyl-substituted PNP-pincer iridium trihydride complex as catalyst. Potassium formate was obtained with turnover number up to 3,500,000 and turnover frequency of 150,000 h^-1.

Journal of the American Chemical Society published new progress about 338800-13-8. 338800-13-8 belongs to pyridine-derivatives, auxiliary class Bis-phosphine Ligands, name is 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, and the molecular formula is C7H13BrSi, Recommanded Product: 2,6-Bis((di-tert-butylphosphino)methyl)pyridine.

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

Fujinaga, Masayuki published the artcileSynthesis and evaluation of 6-[1-(2-[¹⁸F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain, Category: pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry (2011), 19(1), 102-110, database is CAplus and MEDLINE.

The purpose of this study was to synthesize 6-[1-(2-[¹⁸F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline ([¹⁸F]FPTQ, [¹⁸F]7a) and to evaluate its potential as a positron emission tomog. ligand for imaging metabotropic glutamate receptor type 1 (mGluR1) in the rat brain. Compound [¹⁸F]7a was synthesized by [¹⁸F]fluorination of 6-[1-(2-bromo-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline (7b) with potassium [¹⁸F]fluoride. At the end of synthesis, 1280-1830 MBq (n = 8) of [¹⁸F]7a was obtained with >98% radiochem. purity and 118-237 GBq/μmol specific activity using 3300-4000 MBq of [¹⁸F]F^–. In vitro autoradiog. showed that [¹⁸F]7a had high specific binding with mGluR1 in the rat brain. Biodistribution study using a dissection method and small-animal PET showed that [¹⁸F]7a had high uptake in the rat brain. The uptake of radioactivity in the cerebellum was reduced by unlabeled 7a and mGluR1-selective ligand JNJ-16259685 (2), indicating that [¹⁸F]7a had in vivo specific binding with mGluR1. Because of a low amount of radiolabeled metabolite present in the brain, [¹⁸F]7a may have a limiting potential for the in vivo imaging of mGluR1 by PET.

Bioorganic & Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Category: pyridine-derivatives.

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

Yu, Xiao-Qiang published the artcileAryl triolborates: Novel reagent for copper-catalyzed N-arylation of amines, anilines, and imidazoles, Recommanded Product: 2-Pyridinylboronic acid, the publication is Chemistry – An Asian Journal (2008), 3(8-9), 1517-1522, database is CAplus and MEDLINE.

The N-arylation of primary and secondary aliphatic amines, anilines, and imidazoles with novel potassium aryl triolborates was carried out in the presence of a reoxidant and a catalytic amount of Cu(OAc)₂ (10 mol %). Aryl triolborates were found to be better reagents than arylboronic acids or potassium aryl trifluoroborates as the former achieved high yields under mild conditions. Coupling of primary and secondary aliphatic amines to give N-arylamines in excellent yields was performed under oxygen atm. The reactions of anilines and imidazoles to provide N-arylanilines and N-arylimidazoles in good yields proceeded smoothly when trimethylamine N-oxide was used as an oxidant.

Chemistry – An Asian Journal published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is Al2H32O28S3, Recommanded Product: 2-Pyridinylboronic acid.

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

Mikami, Eiichi published the artcileRapid determination of drugs in pharmaceutical preparations by liquid chromatography. (III). Determination of todralazine hydrochloride, trimetoquinol hydrochloride, nicardipine hydrochloride, sulpiride, furosemide and betahistine mesilate in pharmaceutical preparations, Formula: C10H20N2O6S2, the publication is Iyakuhin Kenkyu (1992), 23(6), 896-901, database is CAplus.

Liquid chromatog. methods using UV detection are described for determination of the title drugs in pharmaceutical preparations Stationary phase was Wakosil 5C18. Internal standards were p-hydroxybenzoic acid (for todralazine hydrochloride and sulpiride), Me p-aminobenzoate (for trimetoquinol hydrochloride and betahistidine mesilate), Pr p-hydroxybenzoate (for nicardipine hydrochloride), and Pr p-aminobenzoate (for furosemide). These rapid methods are useful for anal. for com. pharmaceutical preparations

Iyakuhin Kenkyu 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, Formula: C10H20N2O6S2.

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

Kaewchuay, Netnapit published the artcileA novel hybrid mode of sample injection to enhance CZE sensitivity for simultaneous determination of a pyridine-triphenylborane anti-fouling agent and its degradation products, Synthetic Route of 971-66-4, the publication is Electrophoresis (2011), 32(12), 1486-1491, database is CAplus and MEDLINE.

We developed a novel hybrid sample injection mode (HSIM) that presents the combination of electrokinetic injection and vacuum injection to enhance detection sensitivity in CZE. Samples were introduced using both vacuum and electrokinetic injections simultaneously, with a water plug injected into the capillary prior to sample introduction (i.e. similarly to field-amplified sample injection, FASI). Using a sample mixture containing an anti-fouling agent applied to ship hulls, pyridine-triphenylborane and its degradation products (diphenylborinic acid, phenylboronic acid, and phenol) dissolved in ACN, the length of water plug, time, and voltage for sample introduction were optimized. The signal intensity (peak height) was found to be up to a 30-fold increased using HSIM by applying 4 kV for 4 s at the inlet end of the capillary as the cathode with supplementary vacuum in comparison with only vacuum injection for 4 s. The LODs (at a S/N of 3) for pyridine-triphenylborane, diphenylborinic acid, phenylboronic acid, and phenol were 0.88, 1.0, 21, and 23 μg/L, resp. At the level of 0.04 mg/L, the RSDs (n=4, intra-day) for the above analytes were in the ranges of 1.9-11, 4.3-9.2, and 0.34-0.66% for peak area, peak height, and migration time, resp. The HSIM is a simple and promising procedure useful for enhancing the sensitivity for both low-and high-mobility ions in CZE.

Electrophoresis 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, Synthetic Route of 971-66-4.

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

Fukushi, Keiichi published the artcileSimultaneous determination of a pyridine-triphenylborane anti-fouling agent and its estimated degradation products using capillary zone electrophoresis, Application of Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Journal of Chromatography A (2010), 1217(14), 2187-2190, database is CAplus and MEDLINE.

A com. organoborane compound, pyridine-triphenylborane (PTPB), is often applied to ship hulls as an anti-fouling agent. The authors developed capillary zone electrophoresis (CZE) with direct UV detection for the simultaneous determination of PTPB and its estimated degradation products: diphenylborinic acid (DPB), phenylboronic acid (MPB), and phenol. The limits of detection (LODs) for PTPB, DPB, MPB, and phenol were, resp., 25, 30, 50, and 29 μg/L at a signal-to-noise ratio of three. At concentrations of 0.5 mg/L, values of the relative standard deviation (relative standard deviation, n = 6, intra-day) of peak area were obtained, resp., for PTPB, DPB, MPB, and phenol, as 4.1%, 4.1%, 4.7%, and 3.4% for peak heights 3.6%, 3.2%, 1.7%, and 1.4%, and for migration times 1.1%, 1.1%, 1.0%, and 0.73%. The analytes were detected within 14 min. Simple photodegradation experiments were conducted to verify the usefulness of the proposed method for addnl. PTPB degradation studies.

Journal of Chromatography A 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, Application of Triphenyl(pyridin-1-ium-1-yl)borate.

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

Kuznetsov, V. V. published the artcileSpectrophotometric titrimetry of nitrogen-containing heteroaromatic sulfonates in organo-aqueous solutions, Computed Properties of 636-73-7, the publication is Zhurnal Analiticheskoi Khimii (1990), 45(11), 2204-10, database is CAplus.

The formation constants and free energy of transfer of Ba complexes with 8-quinolinol-2-, 8-quinolinol-5-, and 3-pyridinesulfonates in H₂O-Me₂CO were examined by potentiometry and a method was developed for determining the sulfonates in the presence of sulfates. The method involves titration with BaCl₂ vs. Orthanilic B.

Zhurnal Analiticheskoi Khimii published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Computed Properties of 636-73-7.

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

Sreedhar, B. published the artcileNanocrystalline Titania-Supported Palladium(0) Nanoparticles for Suzuki-Miyaura Cross-Coupling of Aryl and Heteroaryl Halides, Computed Properties of 197958-29-5, the publication is Advanced Synthesis & Catalysis (2011), 353(14-15), 2823-2836, database is CAplus.

The Suzuki cross-coupling reaction of various aryl and heteroaryl halides with arylboronic and heteroarylboronic acids was studied using a titania-supported palladium(0) catalyst at room temperature under air. The conversion and selectivity results obtained for many substrates were excellent and similar to those provided by more active or even homogeneous catalysts. The methodol. was similarly effective using 2-bromo-3,4,5-trimethoxybenzaldehyde as the coupling partner. Furthermore, it has been shown that it is useful for the synthesis of terphenyls and tetraphenyls. The catalyst is quant. recovered from the reaction by simple filtration and reused for a number of cycles without significant loss of activity. Inductively coupled plasma (ICP) mass-spectrometric anal. of the filtrate from the reaction mixture demonstrated that the palladium metal hardly leached into the solution within the limits of the detector (1 ppm), thus suggesting that the present Suzuki-Miyaura reaction proceeded by heterogeneous catalysis.

Advanced Synthesis & Catalysis published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C12H9N3O4, Computed Properties of 197958-29-5.

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