Tag: M.W=300-350

Hansen, Christopher J. published the artcileEffects of Solvents, Emulsions, Cosolvents, and Complexions on Ex Vivo Mouse Myometrial Contractility, SDS of cas: 21829-25-4, the publication is Reproductive Sciences (2022), 29(2), 586-595, database is CAplus and MEDLINE.

A great need exists to develop tocolytic and uterotonic drugs that combat poor, labor-related maternal and fetal outcomes. A widely utilized method to assess novel compounds for their tocolytic and uterotonic efficacy is the isometric organ bath contractility assay. Unfortunately, water-insoluble compounds can be difficult to test using the physiol., buffer-based, organ bath assay. Common methods for overcoming solubility issues include solvent variation, cosolvency, surfactant or complexion use, and emulsification. However, these options for drug delivery or formulation can impact tissue function. Therefore, the goal of this study was to evaluate the ability of common solvents, surfactants, cosolvents, and emulsions to adequately solubilize compounds in the organ bath assay without affecting mouse myometrial contractility. We found that acetone, acetonitrile, and ethanol had the least effect, while dimethylacetamide, Et acetate, and isopropanol displayed the greatest inhibition of myometrial contractility based on area under the contractile curve analyses. The min. concentration of surfactants, cosolvents, and human serum albumin required to solubilize nifedipine, a current tocolytic drug, resulted in extensive bubbling in the organ bath assay, precluding their use. Finally, we report that an oil-in-water base emulsion containing no drug has no statistical effect beyond the control (water), while the drug emulsion yielded the same potency and efficacy as the freely solubilized drug.

Reproductive Sciences 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

Cirek, Zdenek published the artcileEfficacy and tolerability of a fixed combination of cinnarizine and dimenhydrinate versus betahistine in the treatment of otogenic vertigo: A double-blind, randomised clinical study, HPLC of Formula: 54856-23-4, the publication is Clinical Drug Investigation (2005), 25(6), 377-389, database is CAplus and MEDLINE.

Introduction: Peripheral vestibular disorders frequently lead to the manifestation of symptoms of vertigo. The objective of this study was to compare the efficacy and tolerability of a fixed combination of cinnarizine 20mg and dimenhydrinate 40mg per tablet with betahistine (betahistine dimesylate) 12mg per tablet in the treatment of patients with otogenic vertigo. Patients and methods: Sixty-one patients with vertigo due to peripheral vestibular disorders (otogenic vertigo) participated in this prospective, double-blind, comparative, single-center study. Patients were randomly allocated to treatment with betahistine 12mg or the fixed combination of cinnarizine 20mg and dimenhydrinate 40mg, both treatments given three times daily for 4 wk. Efficacy was determined by patients’ assessments of vertigo symptoms after 1 and 4 wk of treatment using a visual analog scale to determine a ‘mean vertigo score’. Results: Treatment with the fixed combination led to significantly greater improvements in mean vertigo scores compared with the reference therapy betahistine. This was evident as early as 1 wk after the onset of treatment (p = 0.002). Over 4 wk of therapy, the fixed combination decreased the intensity of vertigo symptoms about 2-fold compared with betahistine (p = 0.001). Furthermore, reductions in symptoms typically associated with vertigo were more pronounced (p = 0.009) in the fixed-combination group compared with the betahistine group after 4 wk of treatment. No serious adverse events were reported in either treatment group. Tolerability of the fixed combination was judged as ‘very good’ by 97% (betahistine 90%) and as ‘good’ by 3% (betahistine 10%) of patients. Conclusion: The fixed combination of cinnarizine and dimenhydrinate was shown to be an effective and very well tolerated treatment option for patients with otogenic vertigo. It proved to be statistically more efficient in reducing vertigo than the widely used betahistine. Therefore, the fixed combination of cinnarizine and dimenhydrinate may be considered a first-line treatment option for the treatment of otogenic vertigo.

Clinical Drug Investigation 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, HPLC of Formula: 54856-23-4.

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

Lee, Seoung Rak published the artcileInduction of Diverse Cryptic Fungal Metabolites by Steroids and Channel Blockers, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Angewandte Chemie, International Edition (2022), 61(29), e202204519, database is CAplus and MEDLINE.

Fungi offer a deep source of natural products but remain underutilized. Most biosynthetic gene clusters (BGCs) that can be detected are silent or “cryptic” in standard lab cultures and their products are thus not interrogated in routine screens. As genetic alterations are difficult and some strains can only be grown on agar, we have herein applied an agar-based high-throughput chem. genetic screen to identify inducers of fungal BGCs. Using R. solani and S. sclerotiorum as test cases, we report 13 cryptic metabolites in four compound groups, including sclerocyclane, a natural product with a novel scaffold. Steroids were the best elicitors and follow-up studies showed that plant-steroids trigger sclerocyclane synthesis, which shows antibiotic activity against B. plantarii, an ecol. competitor of S. sclerotiorum. Our results open new paths to exploring the chem. ecol. of fungal-plant interactions and provide a genetics-free approach for uncovering cryptic fungal metabolites.

Angewandte Chemie, International Edition 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

Eisch, John J. published the artcileRearrangements of organometallic compounds. 26. Bora-aromatic systems. 15. Skeletal rearrangements of arylborane complexes mediated by redox reactions: thermal and photochemical oxidation by metal ions, Application of Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Journal of Organometallic Chemistry (1994), 464(1), 11-21, database is CAplus.

A variety of metal salts are reduced by thermal and photochem. interaction with tetraarylborate salts and with neutral alkyl- and aryl-borane complexes. In the cases of Cu²⁺, Cu⁺, Ni²⁺, Co²⁺, Pd²⁺, Pt²⁺, Ag⁺, Zn²⁺, Hg²⁺, Sn²⁺, Pb²⁺ and Rh³⁺ salts, such photochem. reductions with NaBPh₄ led to the deposition of the free metal, while a number of binary mixtures of metal salts led to the codeposition of both metals, sometimes as true alloys, under such photoreductions The arylborate reductants underwent oxidative coupling of the aryl groups to form biaryls in a strictly intra-ionic (for BAr₄^–) or intramol. (Ar₃B) manner, resp. Individual studies of the photochem. of the tetraarylborate anion itself, of cuprous tetraphenylborate and of the triphenylborane-pyridine complex adduced evidence for a gamut of reactive intermediates capable of serving as the photoreductant for metal ions, such as triarylborane radical anions, diarylborate(I) anions or arylborenes, 7-borabicycloheptadiene anions or neutral complexes and finally arylborohydride anions or arylboron hydrides. The role of these intermediates both in the photoinduced skeletal rearrangements of arylboranes and in the concomitant reduction of metal ions is discussed in critical detail.

Journal of Organometallic 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 C23H20BN, Application of Triphenyl(pyridin-1-ium-1-yl)borate.

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

Mahajan, Abhishek published the artcileInterplay mechanisms between progesterone and endocannabinoid receptors in regulating bull sperm capacitation and acrosome reaction, Synthetic Route of 21829-25-4, the publication is Journal of Cellular Physiology (2022), 237(7), 2888-2912, database is CAplus and MEDLINE.

After ejaculation, sperm show a limited capacity for transcription and translation. In the oviduct, most of the signalling in sperm is nongenomic and is mediated through membrane receptors. Studies have shown that the cation channel of sperm (CatSper), cAMP, cGMP, protein kinases, and tyrosine phosphorylation are involved in the nongenomic signalling of progesterone (P4) in sperm. However, it is not known whether there is an interplay between P4 and cannabinoid receptors 1 and 2 (CB1 and CB2), transient receptor potential vanilloid 1 (TRPV1), CatSper channels, cAMP, inositol trisphosphate receptor (IP3R), and mitogen-activated protein kinase (MAPK); these potential regulators are involved in the regulation of capacitation and the acrosome reaction. In the present study, selective blockers of CB1, CB2, TRPV1, CatSper channels, cAMP, protein kinase A (PKA), IP3R, and MAPK were used to identify their involvement in P4-mediated bull sperm capacitation and the acrosome reaction. Selective blocking of any one of the mols. caused a significant reduction in P4 signalling (p < 0.05). Interestingly, blocking these mols. in combination followed by treatment with P4 resulted in the complete absence of capacitation and the acrosome reaction. Blocking a single receptor was not able to eliminate the P4-induced capacitation and the acrosome reaction. In addition to the CB1 and CB2 receptors, there may be other signalling pathways that mediate P4 signalling. In conclusion, P4 signalling exhibited interplay with the cannabinoid receptors. The regulation of sperm capacitation and the acrosome reaction also involved cAMP, PKA, L-type and T-type calcium channels, TRPV1, inositol trisphosphate, and MAPK.

Journal of Cellular Physiology 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, Synthetic Route of 21829-25-4.

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

Cheng, Ivy published the artcileEffects of pharmacological agents for neurogenic oropharyngeal dysphagia: A systematic review and meta-analysis, Related Products of pyridine-derivatives, the publication is Neurogastroenterology & Motility (2022), 34(3), e14220, database is CAplus and MEDLINE.

This systematic review and meta-anal. aimed to evaluate the effects of pharmacol. agents for neurogenic oropharyngeal dysphagia based on evidence from randomized controlled trials (RCTs). Electronic databases were systematically searched between Jan. 1970 and March 2021. Two reviewers independently extracted and synthesized the data. The outcome measure was changed in (any) relevant clin. swallowing-related characteristics. Data from 2186 dysphagic patients were collected from 14 RCT studies across a range of pharmacotherapies. The pooled effect size of transient receptor potential (TRP) channel agonists was large compared to placebo interventions (SMD[95%CI] =1.27[0.74,1.80], p < 0.001; I2 = 79%). Data were limited for other pharmacol. agents and the overall pooled effect size of these agents was non-significant (SMD [95% CI] =0.25 [-0.24, 0.73]; p = 0.31; I2 = 85%). When analyzed sep., large effect sizes were observed with Nifedipine (SMD[95%CI] =1.13[0.09,2.18]; p = 0.03) and Metoclopramide (SMD[95%CI] =1.68[1.08,2.27]; p < 0.001). By contrast, the effects of angiotensin-converting enzyme (ACE) inhibitors (SMD[95%CI] = -0.67[-2.32,0.99]; p = 0.43; I2 = 61%), Physostigmine (SMD[95%CI] = -0.05[-1.03,0.93]; p = 0.92) and Glyceryl Trinitrate (GTN) (SMD [95% CI] = -0.01 [-0.11, 0.08]; p = 0.78) were non-significant. Within stroke patients, subgroup anal. showed that TRP channel agonists had a moderate pooled effect size (SMD[95%CI] =0.74[0.10,1.39]; p = 0.02; I2 = 82%) whereas the effects of other agents were non-significant (SMD[95%CI] =0.40[-0.04,0.84]; p = 0.07; I2 = 87%). Our results showed that TRP channel agonists, Nifedipine and Metoclopromide may be beneficial for neurogenic dysphagic patients. Large scale, multicenter clin. trials are warranted to fully explore their therapeutic effects on swallowing.

Neurogastroenterology & Motility 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

Mizugaki, Michinao published the artcileExtra-weak chemiluminescence of drugs. I. Extra-weak chemiluminescence of tablets and capsules, Name: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Yakugaku Zasshi (1985), 105(4), 401-6, database is CAplus and MEDLINE.

The measurement of extra-weak chemiluminescence of 139 tablets and capsules was carried out with single photoelectron counting apparatus The tablets and capsules tested showed chemiluminescence values of 0 to 1380 counts/10 s, 0 to 10,800 counts/10 s and 37 to 245,000 counts/10 s, at 20, 50 and 80°, resp. Among the drugs tested in this report, imipramine, indole, and phenothiazine derivatives showed high chemiluminescence values.

Yakugaku Zasshi 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

Anant, Arjun published the artcileAn analytical review for the estimation of montelukast sodium, Related Products of pyridine-derivatives, the publication is Separation Science plus (2022), 5(5), 120-137, database is CAplus.

A review. Montelukast is a highly potent and selective receptor antagonist of cysteinyl leukotrienes (CysLT1) used in chronic asthma and vasoconstriction reduction and also used in allergies, swelling, hay fever, and shortness of breath. For the measurement of montelukast sodium in biol. and pharmaceutical samples, there are different asynchronous and concurrent anal. methods, such as high-performance thin layer chromatog., UV spectroscopy, capillary electrophoresis, high-performance liquid chromatog., and liquid chromatog.-mass spectrometry, have been developed. The pathogenesis of asthma, mechanism of action, and various anal. methods for the detection of montelukast sodium and its combination of dosage forms and biol. samples have been described in the present review. Ranjan et al. suggested the reverse phase high-performance liquid chromatog. approach for estimating montelukast in rabbit plasma and found the best limit of detection result of 1.0 ng/mL. Ezzeldin et al. developed a liquid chromatog. with tandem mass spectrometry system for the simultaneous detection of combinations of montelukast, gliclazide, and nifedipine. The authors conclude that the studies described in the present manuscript will assist researchers in choosing a simple, rapid, and responsive method for the anal. of montelukast sodium and its combinations.

Separation Science plus 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

Narimani, Saeedeh published the artcileMicrowave-assisted facile synthesis of N, P co-doped fluorescent carbon dot probe for the determination of nifedipine., Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Analytical sciences : the international journal of the Japan Society for Analytical Chemistry (2022), 38(2), 393-399, database is MEDLINE.

A simple and fast microwave synthesis method was applied for the preparation of several carbon dots (CDs) from various combinations of urea, phosphoric acid, and B-alanine as nitrogen, phosphorus, and carbon precursors. The maximum quantum yield (44%) was obtained for nitrogen and phosphorus co-doped carbon dots (N, P-CDs) prepared from urea, B-alanine, and phosphoric acid. Furthermore, N, P-CDs were exploited to synthesize a simple and sensitive fluorometric probe to determine nifedipine (NFD). We determined that the analytical response of the designed sensor could be affected by the kind of dopant and synthesis precursors. It is worth mentioning that the fluorescence intensity of N, P-CDs was weakened by NFD, and no fluorescence quenching was observed for other prepared CDs. The NFD-developed sensor demonstrated a linear response range of 3.3 ×â€?0^-8-3.2 ×â€?0^-5 mol/L, with the detection limit of 1.0 ×â€?0^-8 mol/L. The sensor was successfully applied to measure NFD in human biological fluids.

Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 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

Kawabata, Atsuhiko published the artcileEffects of anti-vertigo drugs on medial vestibular nucleus neurons activated by horizontal rotation, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Japanese Journal of Pharmacology (1991), 55(1), 101-6, database is CAplus and MEDLINE.

The effects of anti-vertigo drugs on the brain medial vestibular nucleus (MVN) neurons were examined to assess the site and mode of action using cats anesthetized with α-chloralose. Single neuron activity in the MVN was extracellularly recorded using a silver wire microelectrode filled with diphenhydramine, diphenidol, betahistine, glutamate, or NaCl. Type I of the MVN neurons were identified according to the responses obtained when the animal placed on a turn-table was rotated sinusoidally. The drug effects were examined on type I neurons which received impulses primarily from the labyrinth and sent them to the oculomotor nuclei. The microiontophoretic application of diphenhydramine, diphenidol, and betahistine inhibited the rotation-induced firing of type I MVN neurons. Diphenhydramine and diphenidol were more potent than betahistine. These drugs act directly on MVN neurons and reduce the responsiveness to rotatory stimulation.

Japanese Journal of Pharmacology 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, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate.

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