Category: 54856-23-4

Novotny, Miroslav published the artcileFixed combination of cinnarizine and dimenhydrinate versus betahistine dimesylate in the treatment of Meniere’s disease: a randomized, double-blind, parallel group clinical study, Synthetic Route of 54856-23-4, the publication is International Tinnitus Journal (2002), 8(2), 115-123, database is CAplus.

In a randomized, double-blind clin. study, we evaluated the efficacy and tolerability of the fixed combination of cinnarizine, 20 mg, and dimenhydrinate, 40 mg (Arlevert [ARL]) in comparison to betahistine dimesylate (12 mg) in 82 patients suffering from Meniere’s disease for at least 3 mo and showing the characteristic triad of symptoms (paroxysmal vertigo attacks, cochlear hearing loss, and tinnitus). The treatment (one tablet three times daily) extended to 12 wk, with control visits at 1, 3, 6, and 12 wk after drug intake. The study demonstrated for both the fixed-combination ARL and for betahistine a highly efficient reduction of vertigo symptoms in the course of the 12 wk of treatment; however, no statistically significant difference between the two treatment groups could be established. Similar results were found for tinnitus (approx. 60% reduction) and for the associated vegetative symptoms (almost complete disappearance). Vestibulospinal reactions, recorded by craniocorpog., also improved distinctly, with a statistically significant superiority of ARL vs. betahistine (p <.042) for the parameter of lateral sway (Unterberger’s test). The caloric tests (electronystagmog.) showed only minor changes for both treatment groups in the course of the study. A statistically significant improvement of hearing function of the affected ear (p =.042) was found for the combination preparation after 12 wk of treatment. The tolerability was judged by the vast majority of patients (97.5%) in both groups to be very good. Only one patient (betahistine group) reported a nonserious adverse event, and two betahistine patients did not complete the study. In conclusion, the combination preparation proved to be a highly efficient and safe treatment option for Meniere’s disease and may be used both in the management of acute episodes and in long-term treatment. Efficacy and safety were similar to the widely used standard therapy with betahistine.

International Tinnitus Journal 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, Synthetic Route of 54856-23-4.

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

Schneider, D. published the artcileInfluence of 3 antivertiginous medications on the vigilance of healthy volunteers, Product Details of C10H20N2O6S2, the publication is International Journal of Clinical Pharmacology and Therapeutics (2003), 41(4), 171-181, database is CAplus and MEDLINE.

In the present randomized, comparative, double-blind, 3-way crossover study, possible effects of 3 antivertiginous medications on vigilance were investigated. Thirty healthy volunteers received single doses of a fixed combination of cinnarizine 20 mg and dimenhydrinate 40 mg (Arlevert, ARL), dimenhydrinate 50 mg, or betahistine dimesylate 12 mg, in randomized order at 1-wk intervals. Spontaneous brain elec. activity (EEG), acoustic late evoked potentials (ALEP) with P300, and reaction time were measured before and 90 (t₉₀) and 180 min (t₁₈₀) after drug intake. All 3 medications led to a delay of P300 (primary criterion) and a decrease of its amplitude. The maximum delay at t₁₈₀ was found for dimenhydrinate (16.42 ms) and the lowest for betahistine (6.33 ms). The differences in ARL vs. dimenhydrinate and ARL vs. betahistine were not statistically significant (p > 0.05). Spectral anal. of spontaneous EEG showed slight and similar decreases in the power in the α-band under dimenhydrinate and ARL (p = 0.07 and p = 0.03 with respect to baseline, resp.), but basically no change under betahistine. There was no effect on reaction time by either medication. None of the subjects reported drowsiness or any other adverse event. The findings confirm the reported suitability of P300 latency for measurement of drug effects on brain activity, but provide no indication of concomitant impairment of performance capacity by the tested drugs. Global assessment of the results suggests that the fixed combination cinnarizine 20 mg/dimenhydrinate 40 mg exerts only a minor effect on vigilance, not significantly different from betahistine, which is commonly regarded as a non-sedating antivertiginous drug.

International Journal of Clinical Pharmacology and Therapeutics 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, Product Details of C10H20N2O6S2.

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

Shahar, Or David published the artcileA high-throughput chemical screen with FDA approved drugs reveals that the antihypertensive drug Spironolactone impairs cancer cell survival by inhibiting homology directed repair, Application In Synthesis of 54856-23-4, the publication is Nucleic Acids Research (2014), 42(9), 5689-5701, database is CAplus and MEDLINE.

DNA double-strand breaks (DSBs) are the most severe type of DNA damage. DSBs are repaired by non-homologous end-joining or homol. directed repair (HDR). Identifying novel small mols. that affect HDR is of great importance both for research use and therapy. Mols. that elevate HDR may improve gene targeting, whereas inhibiting mols. can be used for chemotherapy, since some of the cancers are more sensitive to repair impairment. Here, the authors performed a high-throughput chem. screen for FDA approved drugs, which affect HDR in cancer cells. The authors found that HDR frequencies are increased by retinoic acid and Idoxuridine and reduced by the antihypertensive drug Spironolactone. The authors further revealed that Spironolactone impairs Rad51 foci formation, sensitizes cancer cells to DNA damaging agents, to Poly (ADP-ribose) polymerase (PARP) inhibitors and crosslinking agents and inhibits tumor growth in xenografts, in mice. This study suggests Spironolactone as a new candidate for chemotherapy.

Nucleic Acids Research 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 C18H12ClNO, Application In Synthesis of 54856-23-4.

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

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

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

Zhou, Su published the artcileOptimization for the coating prescription of porosity osmotic pump-controlled release tablets of betahistine mesilate, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Zhongguo Yaofang (2011), 22(21), 1970-1972, database is CAplus.

The aim of this paper is to prepare porosity osmotic pump-controlled release tablets of betahistine mesilate, and optimize the coating prescription. Main influencing factors for drug release of porosity osmotic pump-controlled release tablets were investigated with single factor experiment The coating prescription was optimized by orthogonal test with the amount of PEG and DBP as factors and drug release indicator L as index. Similar factor was less than 50 which indicated that the amount of PEG, DBP and coating level affected the in vitro drug release significantly. The optimized coating prescription was as follows: PEG 30%, DBP 20% and the weight increment of coating material 4%. The drug release indicators of 3 batches of samples in validation test were 13.99, 11.15 and 8.37. Accumulative drug release rate was more than 90% within 12 h, and the drug release model showed zero-level drug release characteristics. Porosity osmotic pump-controlled release tablets of betahistine mesilate with optimized prescription can achieve constant complete release in 12 h.

Zhongguo Yaofang 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 C9H8O4, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate.

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

Hughes, Rebecca E. published the artcileMultiparametric High-Content Cell Painting Identifies Copper Ionophores as Selective Modulators of Esophageal Cancer Phenotypes, Synthetic Route of 54856-23-4, the publication is ACS Chemical Biology (2022), 17(7), 1876-1889, database is CAplus and MEDLINE.

Esophageal adenocarcinoma is of increasing global concern due to increasing incidence, a lack of effective treatments, and poor prognosis. Therapeutic target discovery and clin. trials have been hindered by the heterogeneity of the disease, the lack of “druggable” driver mutations, and the dominance of large-scale genomic rearrangements. We have previously undertaken a comprehensive small-mol. phenotypic screen using the high-content Cell Painting assay to quantify the morphol. response to a total of 19,555 small mols. across a panel of genetically distinct human esophageal cell lines to identify new therapeutic targets and small mols. for the treatment of esophageal adenocarcinoma. In this current study, we report for the first time the dose-response validation studies for the 72 screening hits from the target-annotated LOPAC and Prestwick FDA-approved compound libraries and the full list of 51 validated esophageal adenocarcinoma-selective small mols. (71% validation rate). We then focus on the most potent and selective hit mols., elesclomol, disulfiram, and ammonium pyrrolidinedithiocarbamate. Using a multipronged, multitechnol. approach, we uncover a unified mechanism of action and a vulnerability in esophageal adenocarcinoma toward copper-dependent cell death that could be targeted in the future.

ACS Chemical Biology 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, Synthetic Route of 54856-23-4.

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