Tag: M.W=300-350

Maeda, Hideko published the artcileCharacterization of inclusion complexes of betahistine with β-cyclodextrin and evaluation of their anti-humidity properties, Name: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Journal of Inclusion Phenomena and Macrocyclic Chemistry (2016), 86(3-4), 337-342, database is CAplus.

The formation of inclusion complexes between betahistine (BTH) and the β-CD derivatives were investigated. The binding constant (K_c) of the BTH/β-cyclodextrin (β-CD) inclusion complex was determined to be 1400 L/mol based on UV data. The structure of the BTH/β-CD complex in aqueous solution was examined by ¹H-¹H rotating frame nuclear Overhauser effect spectroscopy (ROESY) NMR, and the pyridine ring and side chain moiety of the BTH mol. were found to be inserted from the secondary hydroxyl face of the β-CD. The thermal properties of the solid BTH/β-CD inclusion complexes prepared by kneading and freeze-drying methods were studied by differential scanning calorimetry, and for comparison, solid betahistine mesilate (BTHm)/β-CD inclusion complexes were similarly prepared Humidity tests showed that the solid BTH/β-CD complexes exhibited less moisture absorption compared to the BTHm alone and BTHm/β-CD complexes.

Journal of Inclusion Phenomena and Macrocyclic Chemistry 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, Name: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate.

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

Ishida, Naoki published the artcileSynthesis of Pyridine-N-oxide-Borane Intramolecular Complexes by Palladium-Catalyzed Reaction of 2-Bromopyridine-N-oxides with Alkynyltriarylborates, Application In Synthesis of 971-66-4, the publication is Organic Letters (2011), 13(12), 3008-3011, database is CAplus and MEDLINE.

Pyridine-N-oxide-borane intramol. complexes, e.g., I, having an aza-stilbene π-framework were synthesized by the Pd-catalyzed coupling reactions of 2-bromopyridine-N-oxides with alkynyltriarylborates. E.g., reaction of 2-bromo-5-methoxypyridine-N-oxide and HN(ⁱPr)₂ in toluene at room temperature with [Me₄N][HCCBPh₃] in the presence of [PdCl(π-allyl)]₂/DPEPhos catalyst to give I in 79% yield.

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, Application In Synthesis of 971-66-4.

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

Takeya, Mitsue published the artcilePDGFRα⁺ subepithelial interstitial cells act as a pacemaker to drive smooth muscle of the guinea pig seminal vesicle, Quality Control of 21829-25-4, the publication is Journal of Physiology (Oxford, United Kingdom) (2022), 600(7), 1703-1730, database is CAplus and MEDLINE.

Smooth muscle cells (SMCs) of the guinea pig seminal vesicle (SV) develop spontaneous phasic contractions, Ca2+ flashes and elec. slow waves in a mucosa-dependent manner, and thus it was envisaged that pacemaker cells reside in the mucosa. Here, we aimed to identify the pacemaker cells in SV mucosa using intracellular microelectrode and fluorescence Ca2+ imaging techniques. Morphol. characteristics of the mucosal pacemaker cells were also investigated using focused ion beam/SEM tomog. and fluorescence immunohistochem. Two populations of mucosal cells developed spontaneous Ca2+ transients and elec. activity, namely basal epithelial cells (BECs) and subepithelial interstitial cells (SICs). Pancytokeratin-immunoreactive BECs were located on the apical side of the basement membrane (BM) and generated asynchronous, irregular spontaneous Ca2+ transients and spontaneous transient depolarisations (STDs). The spontaneous Ca2+ transients and STDs were not diminished by 10μM nifedipine but abolished by 10μM cyclopiazonic acid (CPA). Platelet-derived growth factor receptor α (PDGFRα)-immunoreactive SICs were distributed just beneath the basal side of the BM and developed synchronous Ca2+ oscillations and elec. slow waves, which were suppressed by 3μM nifedipine and abolished by 10μM CPA. In SV mucosal preparations in which some smooth muscle bundles remained attached, SICs and residual SMCs developed temporally correlated spontaneous Ca2+ transients. Neurobiotin injected into SICs spread not only to neighboring SICs but also to neighboring SMCs or vice versa. These results suggest that PDGFRα+ SICs electrotonically drive the spontaneous contractions of SV smooth muscle. Key points : In many visceral smooth muscle organs, spontaneous contractions are elec. driven by non-muscular pacemaker cells. In guinea pig seminal vesicles (SVs), as yet unidentified mucosal cells appear to drive neighboring smooth muscle cells (SMCs). Two populations of spontaneously active cells are distributed in the SV mucosa. Basal epithelial cells (BECs) generate asynchronous, irregular spontaneous Ca2+ transients and spontaneous transient depolarisations (STDs). In contrast, subepithelial interstitial cells (SICs) develop synchronous Ca2+ oscillations and elec. slow waves. Pancytokeratin-immunoreactive (IR) BECs are located on the apical side of the basement membrane (BM), while platelet-derived growth factor receptor α (PDGFRα)-IR SICs are located on the basal side of the BM. Spontaneous Ca2+ transients in SICs are synchronised with those in SV SMCs. Dye-coupling between SICs and SMCs suggests that SICs act as pacemaker cells to drive the spontaneous contractions of SV smooth muscle.

Journal of Physiology (Oxford, United Kingdom) 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 C13H9FO2, Quality Control of 21829-25-4.

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

Zhou, Min published the artcileFingerprinting pharmaceuticals of multiple sources at a provincial watershed scale, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Science of the Total Environment (2022), 153356, database is CAplus and MEDLINE.

Pharmaceutical residues in the aquatic environment have increasingly attracted public concerns but their fingerprint of sources remain unclear at a watershed scale. This study systematically explored pharmaceutical residues in effluent of 8 different type of sources in a provincial watershed in China using a multi-category protocol of pharmaceutical quantification. Seventy-seven out of 94 target compounds from 6 categories were quantified in effluent, up to 71,318 ng L^-1 in total from urban hospital sources with 20 antibiotics and 32 others. The spectrum of the quantified compounds in effluent significantly differentiated the urban (hospitals, domestic sewages, and WWTPs), rural (health centers and domestic sewages), and agricultural production sources (poultry and swine breeding yards, aquaculture ponds, and paddy fields). Compounds of non-steroidal anti-inflammation drugs (NSAIDs), cardiovascular drugs (CVs), and central nervous drugs (CNs) could fingerprint the three groups of sources. However, the three categories contributed 7 out of 10 compounds with high risk (risk quotient >1.0) to the aquatic environment identified by the eco-environmental risk assessment. No high-risk compounds were identified in effluent of urban WWTPs. Findings of this study suggest source identification and compound spectrum fingerprinting are crucial for studies on pharmaceutical residues in the aquatic environment, especially the complexity of pharmaceutical residues in source effluents for exploring source-sink dynamics at a watershed scale.

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 C9H12O, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Weber, Jeremy E. published the artcileElectronic and Spin-State Effects on Dinitrogen Splitting to Nitrides in a Rhenium Pincer System, Computed Properties of 971-66-4, the publication is Inorganic Chemistry (2021), 60(9), 6115-6124, database is CAplus and MEDLINE.

Bimetallic nitrogen (N₂) splitting to form metal nitrides is an attractive method for N₂ fixation. Although a growing number of pincer-supported systems can bind and split N₂, the precise relation between the ligand properties and N₂ binding/splitting remains elusive. Here the authors report the first example of an N₂-bridged rhenium(III) complex, [(trans-P₂^tBuPyrr)ReCl₂]₂(μ-η¹:η¹-N₂) (P₂^tBuPyrr = [2,5-(CH₂P^tBu₂)₂C₄H₂N]^–). In this case, N₂ binding occurs at a higher oxidation level than that in other reported pincer analogs. Anal. of the electronic structure through computational studies shows that the weakly π-donor pincer ligand stabilizes an open-shell electronic configuration that leads to enhanced binding of N₂ in the bridged complex. Using SQUID magnetometry, the authors demonstrate a singlet ground state for this Re-N-N-Re complex, and the authors offer tentative explanations for antiferromagnetic coupling of the two local S = 1 sites. Reduction and subsequent heating of the rhenium(III)-dinitrogen complex leads to chloride loss and cleavage of the N-N bond with isolation of the terminal rhenium(V) nitride complex (P₂^tBuPyrr)ReNCl.

Inorganic Chemistry 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 C5H5F3O2, Computed Properties of 971-66-4.

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

Tsunemasa, Noritaka published the artcileContamination of an alternative antifoulant in coastal waters of Hiroshima Bay, Product Details of C23H20BN, the publication is Kankyo Kagaku (2006), 16(2), 201-211, database is CAplus.

It is well known that organotin (OT) compounds, which are used as effective antifouling biocides, have deleterious effects on nontarget marine organisms when released into water from the coatings applied to boat hulls, and environmental studies have indicated OT contamination of the marine environment on a worldwide scale. In Oct. 2001, the International Maritime Organization (IMO) adopted the International Convention on the Control of Harmful Antifouling Systems (AFS Convention), which prohibited the use of OTs as active ingredients in antifouling systems for ships. Following the international restrictions on the use of OT-based antifoulants, paint manufactures have developed many alternative products. In Japan, more than 20 chem. substances have been used or proposed as alternative compounds In the present study, Sea-nine211, KH101, Diuron, Irgarol 1051 and the latters degradation product M1 were investigated in water from Hiroshima Bay. Concentrations of Sea-nine211, Diuron, Irgarol 1051 and M1 in water samples were in the range of <0.023âˆ?.10, <0.040âˆ?.43, <0.092, and <0.031âˆ?.3 μg/L, resp. KH101 was not detected in the water samples.

Kankyo Kagaku 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 C8H10O2, Product Details of C23H20BN.

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

Drumm, Bernard T. published the artcileCa²⁺ signaling in interstitial cells of Cajal contributes to generation and maintenance of tone in mouse and monkey lower oesophageal sphincters, Related Products of pyridine-derivatives, the publication is Journal of Physiology (Oxford, United Kingdom) (2022), 600(11), 2613-2636, database is CAplus and MEDLINE.

The lower oesophageal sphincter (LES) generates tone and prevents reflux of gastric contents. LES smooth muscle cells (SMCs) are relatively depolarised, facilitating activation of Ca_v1.2 channels to sustain contractile tone. We hypothesised that i.m. interstitial cells of Cajal (ICC-IM), through activation of Ca²⁺-activated Cl^– channels (ANO1), set membrane potentials of SMCs favorable for activation of Ca_v1.2 channels. In some gastrointestinal muscles, ANO1 channels in ICC-IM are activated by Ca²⁺ transients, but no studies have examined Ca²⁺ dynamics in ICC-IM within the LES. Immunohistochem. and qPCR were used to determine expression of key proteins and genes in ICC-IM and SMCs. These studies revealed that Ano1 and its gene product, ANO1, are expressed in c-Kit ⁺cells (ICC-IM) in mouse and monkey LES clasp muscles. Ca²⁺ signalling was imaged in situ, using mice expressing GCaMP6f specifically in ICC (Kit-KI-GCaMP6f). ICC-IM exhibited spontaneous Ca²⁺ transients from multiple firing sites. Ca²⁺ transients were abolished by cyclopiazonic acid or caffeine but were unaffected by tetracaine or nifedipine. Maintenance of Ca²⁺ transients depended on Ca²⁺ influx and store reloading, as Ca²⁺ transient frequency was reduced in Ca²⁺ free solution or by Orai antagonist. Spontaneous tone of LES muscles from mouse and monkey was reduced ∼80% either by Ani9, an ANO1 antagonist or by the Ca_v1.2 channel antagonist nifedipine. Membrane hyperpolarisation occurred in the presence of Ani9. These data suggest that intracellular Ca²⁺ activates ANO1 channels in ICC-IM in the LES. Coupling of ICC-IM to SMCs drives depolarisation, activation of Ca_v1.2 channels, Ca²⁺ entry and contractile tone.

Journal of Physiology (Oxford, United Kingdom) 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, Related Products of pyridine-derivatives.

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

Romano, Sonia published the artcileDrug shortages in community pharmacies: Impact on patients and on the health system, Quality Control of 21829-25-4, the publication is Journal of the American Pharmacists Association (2022), 62(3), 791-799.e2, database is CAplus and MEDLINE.

Worldwide, drug shortages are a critical public health concern. Consequences range from inconvenience and distress to more serious concerns related to neg. clin., humanistic and economic outcomes. This study aimed to investigate the impact of drug shortages at the community pharmacies on patients and on the health system in Portugal. A national, cross-sectional, multicenter study was conducted in Portuguese community pharmacies during Apr. 2019. The proportion of patients reporting drug shortages, types of drugs affected and consequent economic burden to patients and the health system were estimated Regional and urban setting stratification was performed.A total of 71.1% of pharmacies participated in the study and 22,830 patient surveys were retrieved. About 52.2% of patients experienced a drug shortage in the past 12 mo; 21.5% had to see a physician to change the prescription and 5.7% declared treatment discontinuation because of this shortage. The estimated economic impact of shortages related to addnl. physician appointments varied between euro2.1-euro4.4 million for patients and euro35.3-euro43.8 million for the National Health Service. Drug shortages were mostly felt in rural and inner regions and least felt in the islands. This national study showed that community pharmacy drug shortages are a national problem with neg. consequences on patients and the health system, which need to be tackled and mitigated.

Journal of the American Pharmacists Association 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

Feng, Yufei published the artcileRelative bioavailability of betahistine mesylate tablet in healthy volunteers, Related Products of pyridine-derivatives, the publication is Zhongguo Linchuang Yaolixue Zazhi (2006), 22(3), 188-191, database is CAplus.

The bioavailability of domestic and imported betahistine mesylate and its bioequivalence in healthy volunteers were studied. A single oral dose of 24 mg domestic and imported betahistine mesylate tablets were given to 20 healthy male volunteers according to an open randomized 2 way crossover design. Plasma concentration of betahistine mesylate was determined by HPLC-MS-MS method. The pharmacokinetic parameter of the two products were as follow: t_max were (1.1 ± 0.5) and (1.0 ± 0.4) h; C_max were (358.88 ± 93.44) and (360.99 ± 62.88) ng/mL^-1; AUC_0-t were (1687.01 ± 400.51) and (1591.43 ± 352.05) ng/h/mL^-1, resp. The relative bioavailability of domestic product was (108.3 ± 24.1)%. The result demonstrated that two formations were bioequivalence by anal. of variance, two-one side test and 90% confidential internal.

Zhongguo Linchuang Yaolixue Zazhi 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

Tomita, M. published the artcileComparative responses of the carotid and vertebral arterial systems of rhesus monkeys to betahistine, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Stroke (1978), 9(4), 382-7, database is CAplus and MEDLINE.

Following i.v. administration of betahistine mesylate (I) [54856-23-4], the mean transit times of blood through the carotid and vertebral arteries were equally shortened by 10%, despite a 20% decrease in the mean arterial blood pressure. The cerebral tissue and cerebellar tissue blood flow was increased by I 70.4-81.4 and 73.2-84.0 mL/100g/min, resp. Since histamine has been reported to produce a decrease in cardiac output, the increase in cerebral blood flow confirmed that I is a selective cerebral vasodilating agent. However, by comparing the hemodynamic data for the 2 cerebral arterial systems, the responses of the carotid and vertebral arterial systems to the vasodilating action of I were essentially the same.

Stroke 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 C7H9BO3S, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate.

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