Tag: M.W=300-350

Oliveira, Isabel B. published the artcileAcute toxicity of tralopyril, capsaicin and triphenylborane pyridine to marine invertebrates, Safety of Triphenyl(pyridin-1-ium-1-yl)borate, the publication is Ecotoxicology (2014), 23(7), 1336-1344, database is CAplus and MEDLINE.

A need for environmentally acceptable alternative antifouling (AF) biocides has arisen through restrictions in the use of many common biocides in the European Union through the Biocidal Product Regulation (Regulation EU Number 528/2012). Three such alternatives are triphenylborane pyridine (TPBP), tralopyril and capsaicin. This study aims at extending the available information on the toxicity of these three emerging AF biocides to key marine invertebrates. Here we investigate the toxicity of tralopyril and capsaicin to the early life stages of the mussel Mytilus galloprovincialis and the sea urchin Paracentrotus lividus and also of tralopyril, capsaicin and TPBP to the early life stages of the copepod Tisbe battagliai. The EC₅₀ that causes abnormal development of mussel’s D-veliger larvae and impairs the growth of sea urchin pluteus larvae are resp. 3.1 and 3.0 μg/L for tralopyril and 3,868 and 5,248 μg/L for capsaicin. Regarding the copepod T. battagliai, the LC₅₀ was 0.9 μg/L for tralopyril, 1,252 μg/L for capsaicin and 14 μg/L for TPBP. The results obtained for the three substances are compared to a reference AF biocide, tributyltin (TBT), and their ecol. risk evaluated. These compounds pose a lower environmental risk than TBT but still, our results suggest that tralopyril and TPBP may represent a considerable threat to the ecosystems.

Ecotoxicology 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, Safety of Triphenyl(pyridin-1-ium-1-yl)borate.

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

Wendt, Ida published the artcileEffects of Five Antifouling Biocides on Settlement and Growth of Zoospores from the Marine Macroalga Ulva lactuca L., Product Details of C23H20BN, the publication is Bulletin of Environmental Contamination and Toxicology (2013), 91(4), 426-432, database is CAplus and MEDLINE.

Antifouling biocides are found in the marine ecosystem were they can affect non-target organisms. In this study the effects of five antifouling biocides on the settlement and growth of Ulva lactuca zoospores were investigated. The biocides investigated were copper (Cu²⁺), 4,5-dichloro-2-n-octyl-3(2H)-isothiazolone (DCOIT), triphenylborane pyridine (TPBP), tolylfluanid and medetomidine. Full concentration-response curves where determined for each compound EC₅₀ values were determined for copper, DCOIT, TPBP and tolylfluanid, all of which inhibited settlement and growth in a concentration dependent manner with the following toxicity ranking; tolylfluanid (EC₅₀ 80 nmol L^-1) âˆ?DCOIT (EC₅₀ 83 nmol L^-1) > TPBP (EC₅₀ 400 nmol L^-1) > Cu²⁺ (EC₅₀ 2,000 nmol L^-1). Medetomidine inhibited settlement and growth only at the extreme concentration of 100,000 nmol L^-1 (93 % effect). The low toxicity is possibly a consequence of a lack of receptors that medetomidine can bind to in the U. lactuca zoospores.

Bulletin of Environmental Contamination and Toxicology 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 C25H47NO8, Product Details of C23H20BN.

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

Peeters, Laura E. J. published the artcileDevelopment and Validation of a Dried Blood Spot Assay Using UHPLC-MS/MS to Identify and Quantify 12 Antihypertensive Drugs and 4 Active Metabolites: Clinical Needs and Analytical Limitations, Formula: C17H18N2O6, the publication is Therapeutic Drug Monitoring (2022), 44(4), 568-577, database is CAplus and MEDLINE.

As nonadherence to antihypertensive drugs (AHDs) can increase the risk of cardiovascular events, hospitalization, and higher costs, there is a need for a reliable, objective, and easy method to assess nonadherence in patients. The dried blood spot (DBS) sampling method used to measure drug concentrations meets these requirements. For detecting nonadherence, identification is more important than quantification. Owing to their use in clin. practice, it is important to measure multiple AHDs with a single method. Therefore, we developed and validated a single DBS method for 17 commonly used AHDs and 4 active metabolites using ultrahigh performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS). Anal. validation of the DBS assay was performed in accordance with the guidelines on bioanal. method validation of the European Medicines Agency and US Food and Drug Administration as well as the International Association of Therapeutic Drug Monitoring and Clin. Toxicol. guidelines. We validated 12 of the 17 AHDs according to the European Medicines Agency and Food and Drug Administration requirements for bioanal. method validation. Eleven AHDs were validated for both identification and quantification of drug concentrations, whereas nifedipine was only validated for identification. However, 5 of the 17 AHDs were excluded due to suboptimal validation results. Lercanidipine was excluded due to nonlinearity, and all 4 AHDs measured in the neg. mode of UHPLC-MS/MS were not in accordance with one or more of the acceptance criteria and were therefore excluded. The described method accurately measured AHDs in DBS and can be used to determine nonadherence in patients. However, method validation revealed a challenging balance between anal. limitations and clin. needs when analyzing multiple drugs using the same method.

Therapeutic Drug Monitoring 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, Formula: C17H18N2O6.

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

Hollingworth, Samantha A published the artcileAntihypertensive medicine use differs between Ghana and Nigeria., Quality Control of 21829-25-4, the publication is BMC cardiovascular disorders (2022), 22(1), 368, database is MEDLINE.

BACKGROUND: Non-communicable diseases are a growing burden in many African countries; cardiovascular disease is the main disease. Antihypertensive medicines (AHM) are a common treatment option but we know little about community use in most low- and medium-income countries (LMIC). We aimed to describe the use of antihypertensive medicines (AHM) in Ghana and Nigeria using a novel data source. METHODS: We used data from mPharma-a health and pharmaceutical company which distributes pharmaceuticals to hospital and retail pharmacies. We extracted data using the anatomical therapeutic chemical (ATC) classification codes and calculated use in defined daily doses and explored patterns by class, medicines, dose, and originator or generic product. RESULTS: AHM use differed between Ghana and Nigeria. The most used classes in Ghana were angiotensin receptor blockers (ARB) followed by calcium channel blockers (CCB) and angiotensin-converting-enzyme inhibitors (ACEi). The five most used products were 16 mg candesartan, 30 mg nifedipine, 10 mg lisinopril, 5 mg amlodipine and 50 mg losartan. In Nigeria ARB, CCB and diuretics were widely used; the top five products were 50 mg losartan, 10 mg lisinopril, 30 mg nifedipine, 40 mg furosemide, and 5 mg amlodipine. More originator products were used in Ghana than Nigeria. CONCLUSION: The differences between Ghana and Nigeria may result from a combination of medical, contextual and policy evidence and reflect factors related to clinical guidance (e.g. standard treatment guidelines), accessibility to prescribers and the role of community pharmacies, and structure of the health system and universal health coverage including funding for medicines. We show the feasibility of using novel data sources to gain insights on medicines use in the community.

BMC cardiovascular disorders 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

Maafi, Mounir published the artcilePhotokinetics of Dacarbazine and Nifedipine under polychromatic light irradiation and their application as new reliable actinometers for the ultraviolet range, Related Products of pyridine-derivatives, the publication is Scientific Reports (2022), 12(1), 7622, database is CAplus and MEDLINE.

The photokinetic behavior of drugs driven by polychromatic light is an area of pharmaceutics that has not received a lot of attention. Most often, such photokinetic data is treated by thermal kinetic models (i.e., the classical 0th-, 1st- or 2nd-order equations). Such models were not anal. derived from the rate-laws of the photodegradation reactions. Polychromatic light kinetic modeling is hence of importance, as a means to providing adequate toolkits and metrics. This paper aims at proposing two reliable drug-actinometers useful for polychromatic UVA range. The general actinometric methodol. offered here is also useful for any drugs/materials obeying a primary photoprocess where both reactant and photoproduct absorb the incident light, of the AB(1φ)εB≠0 type. The present method has been consolidated by the η-order kinetics. This framework further demonstrated the lamp-specificity of actinometers. Overall, Dacarbazine and Nifedipine photodegradations obeyed η-order kinetics, and stand as effective actinometers that can be recommended for the ICH Q1b photostability testing.

Scientific Reports 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

DiMauro, Erin F. published the artcileApplication of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective Na_V1.7 Inhibitors, Product Details of C15H23BClNO3, the publication is Journal of Medicinal Chemistry (2016), 59(17), 7818-7839, database is CAplus and MEDLINE.

The majority of potent and selective hNa_V1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNa_V1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNa_V1.5. Representative lead I demonstrates selectivity over other human Na_V isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

Journal of Medicinal Chemistry published new progress about 1387634-81-2. 1387634-81-2 belongs to pyridine-derivatives, auxiliary class Boronate Esters,Boronate Esters,Boronic acid and ester,Boronic acid and ester, name is 3-Chloro-2-isobutoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, and the molecular formula is C15H23BClNO3, Product Details of C15H23BClNO3.

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

Hashemi, Marzieh published the artcileEnhancing the Anticonvulsant Effects of Nifedipine in Rats Through Encapsulation with Water-Soluble β-Cyclodextrin Polymer, Related Products of pyridine-derivatives, the publication is Pharmaceutical Chemistry Journal (2022), 55(10), 1023-1027, database is CAplus.

Encapsulation is one of the efficient methods recently developed for improving drug delivery. The present study was designed to encapsulate nifedipine (NIF) by water-soluble β-cyclodextrin polymer (β-CDP) and to evaluate the effects of this carrier on NIF-induced anticonvulsant effects. Adult male Wistar rats weighting 200 – 250 g (n = 7) received NIF or encapsulated NIF (β-CDP/NIF) (5, 10 and 20 mg/kg, i.p.), diazepam (2 mg/kg, i.p. as pos. control), and vehicle. Then, pentylenetetrazol (PTZ, 80 mg/kg, i.p.) was injected about 30 min after the drug injection. Changes in the onset time of seizures and duration of their different stages (tonic and tonic-clonic) and total convulsions duration, percentage mortality and percentage of seizure protection were assessed in all test groups. Latency of the seizure onset and duration of tonic and tonic-clonic seizures were significantly decreased in β-CDP/NIF group in comparison with NIF-treated rats (p < 0.05). On the other hand, percentage mortality was significantly decreased and percentage protection was increased by β-CDP/NIF in comparison to NIF (p < 0.05). Therefore, it was concluded that the encapsulation of NIF by β-CDP led to enhancement of the anticonvulsant effects of NIF in rats.

Pharmaceutical Chemistry Journal 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

Principe, Daniel R. published the artcileCalcium channel blockers potentiate gemcitabine chemotherapy in pancreatic cancer, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Proceedings of the National Academy of Sciences of the United States of America (2022), 119(18), e2200143119, database is CAplus and MEDLINE.

There is currently no effective treatment for pancreatic ductal adenocarcinoma (PDAC). While palliative chemotherapy offers a survival benefit to most patients, nearly all will eventually progress on treatment and long-term survivability remains poor. Given the lack of subsequent line treatment options, in this study, we sought to identify novel strategies to prevent, delay, or overcome resistance to gemcitabine, one of the most widely used medications in PDAC. Using a combination of single-cell RNA sequencing and high-throughput proteomic anal., we identified a subset of gemcitabine-resistant tumor cells enriched for calcium/calmodulin signaling. Pharmacol. inhibition of calcium-dependent calmodulin activation led to the rapid loss of drug-resistant phenotypes in vitro, which addnl. single-cell RNA sequencing identified was due to impaired activation of the RAS/ERK signaling pathway. Consistent with these observations, calcium chelation or depletion of calcium in the culture media also impaired ERK activation in gemcitabine-resistant cells, and restored therapeutic responses to gemcitabine in vitro. We observed similar results using calcium channel blockers (CCBs) such as amlodipine, which inhibited prosurvival ERK signaling in vitro and markedly enhanced therapeutic responses to gemcitabine in both orthotopic xenografts and transgenic models of PDAC. Combined, these results offer insight into a potential means of gemcitabine resistance and suggest that select CCBs may provide a clin. benefit to PDAC patients receiving gemcitabine-based chemotherapy.

Proceedings of the National Academy of Sciences of the United States of America 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

Brecklinghaus, Tim published the artcileThe hepatocyte export carrier inhibition assay improves the separation of hepatotoxic from non-hepatotoxic compounds, COA of Formula: C17H18N2O6, the publication is Chemico-Biological Interactions (2022), 109728, database is CAplus and MEDLINE.

An in vitro/in silico method that determines the risk of human drug induced liver injury in relation to oral doses and blood concentrations of drugs was recently introduced. This method utilizes information on the maximal blood concentration (Cmax) for a specific dose of a test compound, which can be estimated using physiol.-based pharmacokinetic modeling, and a cytotoxicity test in cultured human hepatocytes. In the present study, we analyzed if the addition of an assay that measures the inhibition of bile acid export carriers, like BSEP and/or MRP2, to the existing method improves the differentiation of hepatotoxic and non-hepatotoxic compounds Therefore, an export assay for 5-chloromethylfluorescein diacetate (CMFDA) was established. We tested 36 compounds in a concentration-dependent manner for which the risk of hepatotoxicity for specific oral doses and the capacity to inhibit hepatocyte export carriers are known. Compared to the CTB cytotoxicity test, substantially lower EC10 values were obtained using the CMFDA assay for several known BSEP and/or MRP2 inhibitors. To quantify if the addition of the CMFDA assay to our test system improves the overall separation of hepatotoxic from non-hepatotoxic compounds, the toxicity separation index (TSI) was calculated We obtained a better TSI using the lower alert concentration from either the CMFDA or the CTB test (TSI: 0.886) compared to considering the CTB test alone (TSI: 0.775). In conclusion, the data show that integration of the CMFDA assay with an in vitro test battery improves the differentiation of hepatotoxic and non-hepatotoxic compounds in a set of compounds that includes bile acid export carrier inhibitors.

Chemico-Biological Interactions 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, COA of Formula: C17H18N2O6.

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

Held, Katharina published the artcilePharmacological properties of TRPM3 isoforms are determined by the length of the pore loop, Application of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is British Journal of Pharmacology (2022), 179(14), 3560-3575, database is CAplus and MEDLINE.

Background and Purpose : Transient receptor potential melastatin 3 (TRPM3) is a non-selective cation channel that plays a pivotal role in the peripheral nervous system as a transducer of painful heat signals. Alternative splicing gives rise to several TRPM3 variants. The functional consequences of these splice isoforms are poorly understood. Here, the pharmacol. properties of TRPM3 variants arising from alternative splicing in the pore-forming region were compared. Exptl. Approach : Calcium microfluorimetry and patch clamp recordings were used to compare the properties of heterologously expressed TRPM3α1 (long pore variant) and TRPM3α2-α6 (short pore variants). Furthermore, site-directed mutagenesis was done to investigate the influence of the length of the pore loop on the channel function. Key Results : All short pore loop TRPM3α variants (TRPM3α2-α6) were activated by the neurosteroid pregnenolone sulfate (PS) and by nifedipine, whereas the long pore loop variant TRPM3α1 was insensitive to either compound In contrast, TRPM3α1 was robustly activated by clotrimazole, a compound that does not directly activate the short pore variants but potentiates their responses to PS. Clotrimazole-activated TRPM3α1 currents were largely insensitive to established TRPM3α2 antagonists and were only partially inhibited upon activation of the μ opioid receptor. Finally, by creating a set of mutant channels with pore loops of intermediate length, we showed that the length of the pore loop dictates differential channel activation by PS and clotrimazole. Conclusion and Implications : Alternative splicing in the pore-forming region of TRPM3 defines the channel’s pharmacol. properties, which depend critically on the length of the pore-forming loop.

British Journal of Pharmacology 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, 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