Month: December 2022

Wakabayashi, Kohei published the artcileAcute myocardial infarction caused by persistent coronary spasm associated with high-grade macrophage accumulation., Category: pyridine-derivatives, the main research area is clinical diagnostic tests; ischaemic heart disease.

The mechanisms responsible for persistent and lethal coronary spasm remain incompletely understood. Our group treated a patient with non-ST-elevation myocardial infarction (MI) caused by a spontaneously persistent spasm associated with high-grade macrophage accumulation. A 48-year-old man was transferred to an emergency room because of persisted chest tightness. The patient’s chest pain subsided without ST elevation when he arrived at the hospital, but he tested positive for fatty acid-binding protein. Emergent coronary angiography revealed a subtotal occlusion in the middle of the right coronary artery. The occluded lesion was released immediately after an injection of isosorbide dinitrate. No disruption, ulceration or erosion was observed at the culprit lesion segment on optical coherence tomography. The only finding was high-grade macrophage accumulation in the segment of the persistent focal coronary spasm. The present case suggests that the early stage of atherosclerosis with high-grade macrophage accumulation was associated with persistent coronary spasm resulting in acute MI.

BMJ case reports published new progress about clinical diagnostic tests; ischaemic heart disease. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Salama, Mohamed published the artcileMethyldopa versus nifedipine or no medication for treatment of chronic hypertension during pregnancy: A multicenter randomized clinical trial., Application In Synthesis of 21829-25-4, the main research area is Chronic hypertension; Fetal outcome; Maternal outcome; Methyldopa; Nifedipine.

OBJECTIVE: To assess the maternal and fetal outcome in women with mild to moderate chronic hypertension on antihypertensive drug (methyldopa or nifedipine) therapy compared to no medication. METHODS: This multicenter randomized clinical trial was conducted at Menoufia University hospital, Shibin El-kom Teaching hospital and 11 Central hospitals at Menoufia governorate, Egypt.490 pregnant women with mild to moderate chronic hypertension were randomized into three groups; methyldopa group (n��66), nifedipine group (n��60) and control or no medication group (n��64) who were followed from the beginning of pregnancy till the end of puerperium to record maternal and fetal outcome. RESULTS: Mothers in the control (no medication) group were more prone for the development of severe hypertension, preeclampsia, renal impairment, ECG changes, placental abruption and repeated hospital admissions (p��.001) when compared to mothers in both treatment groups (methyldopa and nifedipine). Neonates in the control (no medication) group were more prone for prematurity and admission to neonatal ICU (p��.001). CONCLUSION: Antihypertensive drug therapy is advisable in mild to moderate chronic hypertension during pregnancy to decrease maternal and fetal morbidity. When considering which agents to use for treatment, oral methyldopa and nifedipine are valid options.

Pregnancy hypertension published new progress about Chronic hypertension; Fetal outcome; Maternal outcome; Methyldopa; Nifedipine. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Application In Synthesis of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Tony Y. published the artcileRegioselective synthesis of 2-chloro-3-pyridinecarboxylates, COA of Formula: C6H7ClN2, the main research area is chloropyridinecarboxylate regioselective preparation; pyridinecarboxylate chloro regioselective preparation.

2-Chlorocyanoacetate undergoes base-catalyzed Michael addition to α,β-unsaturated ketones or aldehydes, e.g., acrolein, to afford 5-oxopentenenitrile derivatives, e.g., OHCCH2CH2CCl(CN)CO2Et. In the presence of anhydrous HCl, these compounds cyclize to yield 2-chloro-3-pyridinecarboxylates, e.g., I. The process is highly regiospecific and useful in the synthesis of 2,3-disubstituted pyridines.

Tetrahedron published new progress about chloropyridinecarboxylate regioselective preparation; pyridinecarboxylate chloro regioselective preparation. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, COA of Formula: C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yuan, Yanbing published the artcileRapid detection of illegally added nifedipine in Chinese traditional patent medicine by surface-enhanced Raman spectroscopy., Product Details of C17H18N2O6, the main research area is Chinese traditional patent medicine; Illegal addition; Nanoparticles; Nifedipine; Surface-enhanced Raman spectroscopy.

Nifedipine is an antihypertensive chemical. The illegal addition of this chemical into Chinese traditional patent medicine (CTPM) is unstandardized and lacks regulation. It could bring serious side effects to patients, causing various symptoms. Therefore, accurate detection of nifedipine is very important for human health and the prevention of illegal additives. Surface-enhanced Raman spectroscopy (SERS) is a fast and sensitive fingerprint spectroscopic technique, which has been shown to be promising in drug detection. In this study, nifedipine in CTPM was determined qualitatively and quantitatively with SERS. Linear relationships between the concentrations of nifedipine and the intensities of the characteristic peaks were established. The results showed a linear relationship within the concentration range of 0.5-10 mg/L, and the lowest detectable concentration of nifedipine in CTPM was 0.1 mg/L (equivalent to 0.03% doping of nifedipine in CTPM). This method has shown a great potential in the detection of drugs illegally added to CTPM.

Analytical sciences : the international journal of the Japan Society for Analytical Chemistry published new progress about Chinese traditional patent medicine; Illegal addition; Nanoparticles; Nifedipine; Surface-enhanced Raman spectroscopy. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kametani, Tetsuji published the artcileSyntheses of heterocyclic compounds. CCCLXXI. Synthetic approach to camptothecin, SDS of cas: 21190-89-6, the main research area is camptothecin analog; indolizinoquinoline; quinoline indolizino; pyrrolidinopyridone; pyridone pyrrolidino.

Picolinic acid 1-oxide was esterified with SOCl2 and EtOH to the Et ester, whose treatment with phosphoryl chloride gave Et 6-chloropicolinate (I). Hydrolysis of I with HCl gave 6-oxo-1,6-dihydropicolinic acid (II). Simultaneous condensation and cyclization of the Me ester of II with Me acrylate in the presence of sodium carbonate in DMF yielded the Me, 1,2,3,5-tetrahydro-1,5-dioxoindolizine-2-carboxylate (III). Hydrolysis and decarboxylation of III with HCl gave 3-oxo-pyrrolidino[2,1-f]-2-pyridone (IV). Friedlaender condensation of IV with 2-aminobenzaldehyde gave a camptothecin analog, 9,11-dihydro-9-oxoindolizino[1,2-b]quinoline (V).

Tetrahedron published new progress about camptothecin analog; indolizinoquinoline; quinoline indolizino; pyrrolidinopyridone; pyridone pyrrolidino. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, SDS of cas: 21190-89-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Engin, Seckin published the artcileThe inhibitory effect of trimetazidine on detrusor contractility – a potential repositioning of trimetazidine for the treatment of overactive bladder., Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is calcium; detrusor; fura-2; ion channels; isolated tissue bath; trimetazidine.

OBJECTIVES: This study aimed to identify the effect of trimetazidine (TMZ), an antianginal drug, on detrusor smooth muscle (DSM) contractility and its possible mechanisms of action. METHODS: We performed in-vitro contractility studies on isolated mouse DSM strips and investigated the effect of TMZ on Ca2+ levels in fura-2-loaded A7r5 cells. KEY FINDINGS: TMZ (300 or 1000 µM) inhibited carbachol (CCh)- and KCl-induced contractions and produced a concentration-dependent (10-1000 µM) relaxation in KCl-precontracted DSM strips. TMZ-induced relaxation was markedly decreased by BaCl2, an inward-rectifying K+ channel blocker, but was not altered by preincubation with tetraethylammonium, glibenclamide, 4-aminopyridine, propranolol, L-NAME or methylene blue. TMZ (300 or 1000 µM) reduced both the CaCl2-induced contraction of depolarized DSM strips under Ca2+-free conditions and the CCh-induced contraction of DSM strips preincubated with nifedipine in Ca2+-containing Krebs solution. Furthermore, TMZ (1000 µM) significantly decreased the Ca2+ levels in fura-2-loaded A7r5 cells. CONCLUSIONS: TMZ decreased DSM contractility and caused a concentration-dependent relaxation of the tissue possibly through its actions on Ca2+ transients and K+ channels. Our results provide preclinical evidence that TMZ would be a potential candidate to treat disorders related to the overactivity of the bladder.

The Journal of pharmacy and pharmacology published new progress about calcium; detrusor; fura-2; ion channels; isolated tissue bath; trimetazidine. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Archana, G. M. published the artcileAssays for L-type voltage gated calcium channels, Synthetic Route of 21829-25-4, the main research area is Calcium imaging; Drug discovery; End-point assay for calcium channel; HEK-293; L-type voltage gated calcium channel; VGCC assay.

Voltage gated calcium channels (VGCCs) are pursued as drug targets for neurodegenerative and cardiovascular diseases. High throughput drug screening targeting VGCCs depends on patch-clamp electrophysiol. or fluorophore-based calcium imaging that requires powerful equipment and specialized expertise thus leading to cost escalation. Moreover, VGCC needs to be transfected into cell lines such as HEK-293. We report the presence of L-type VGCC (L-VGCC) subunit proteins, Cav1.2, α2δ and β in HEK-293 cells and the application of simple methods for its assay. Endogenous expression of the channel in HEK-293 cells overcomes the need for transfection. L-VGCC in HEK-293 cells was activated either by the agonist, BayK8644 or by KCl-mediated depolarization. Activity was detected using the calcium sensing probe, GCaMP6m by live imaging. L-VGCC activity induced enhancement in GCaMP6m fluorescence returned to baseline corresponding to channel-closure. Activity was also shown using a methodol. involving end-point detection of the calcium dependent interaction of α-CaMKII with NMDA receptor subunit GluN2B sequence. This methodol. further simplifies the assay as it eliminates the need for real time imaging. Activation was blocked by the specific L-type VGCC antagonist, nifedipine. Finding the protein and activity of L-VGCC in HEK-293 cells offers com. viable assays for drug screening.

Analytical Biochemistry published new progress about Calcium imaging; Drug discovery; End-point assay for calcium channel; HEK-293; L-type voltage gated calcium channel; VGCC assay. 21829-25-4 belongs to class pyridine-derivatives, 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:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kim, Sung Eun published the artcileComparison of calcium-channel blockers for long-term clinical outcomes in patients with vasospastic angina., COA of Formula: C17H18N2O6, the main research area is Calcium channel blockers; Coronary vasospasm; Patient outcome assessment.

BACKGROUND/AIMS: Calcium channel blockers (CCBs) are the most widely prescribed medication for patients with vasospastic angina (VA). However, few studies have compared the prognosis of VA patients who are prescribed different CCBs. METHODS: We enrolled 2,960 patients who received provocation test prospectively in 11 university hospitals in Korea. We divided 1,586 patients received four major CCBs into two groups: a first generation CCB (diltiazem and nifedipine) group and a second generation CCB (amlodipine and benidipine) group. Primary outcome was time to events of composite of death from any cause, acute coronary syndrome (ACS) and symptomatic arrhythmia during 3-year follow-up. We also compared the effect of each CCB on the control of angina symptoms. RESULTS: There was no difference of the primary outcome among the two groups with a cumulative incidence rate of 5.4%, 2.9%, and a person-month incidence rate of 2.33 and 1.26, respectively (hazard ratio [HR], 0.54; 95% confidence interval [CI], 0.25 to 1.17; p = 0.120, as reference with the 1st generation CCBs). The incidence of ACS was significantly lower in 2nd generation CCBs group with a person-month incidence rate of 1.66 vs. 0.35 (HR, 0.22; 95% CI, 0.05 to 0.89; p = 0.034). Use of benidipine showed a significant better control of angina symptom compared with diltiazem for 3 years (odds ratio, 0.17; 95% CI, 0.09 to 0.32; p < 0.0001 at 3rd year). CONCLUSION: The first and second generation CCB groups did not differ in terms of composite outcome occurrence. However, the ACS incidence rate was significantly lower in the users of the 2nd generation CCBs. The Korean journal of internal medicine published new progress about Calcium channel blockers; Coronary vasospasm; Patient outcome assessment. 21829-25-4 belongs to class pyridine-derivatives, 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:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Milliner, Brendan H A published the artcileEffect of Calcium-Channel Blockade on the Cold-Induced Vasodilation Response., Computed Properties of 21829-25-4, the main research area is calcium channel blockers; cold injury; environmental medicine; prevention and control.

INTRODUCTION: Cold-induced vasodilation (CIVD) is seen in the extremities during exposure to cold. A strong vasodilation response has been associated with a decreased risk of cold injury. Increasing CIVD might further decrease this risk. The calcium-channel blocker nifedipine causes vasodilation and is used to treat Raynaud’s syndrome and chilblains. Nifedipine is also used for high altitude pulmonary edema and could potentially serve a dual purpose in preventing frostbite. The effects of nifedipine on CIVD have not been studied. METHODS: A double-blind crossover study comparing nifedipine (30 mg SR (sustained release) orally twice daily) to placebo was designed using 2 sessions of 4 finger immersion in 5°C water, with 24 h of medication pretreatment before each session. Finger temperatures were measured via nailbed thermocouples. The primary outcome was mean finger temperature; secondary outcomes were mean apex and nadir temperatures, first apex and nadir temperatures, subjective pain ranking, and time of vasodilation onset (all presented as mean±SD). RESULTS: Twelve volunteers (age 29±3 [24-34] y) completed the study. No significant difference in finger temperature (9.2±1.1°C nifedipine vs 9.0±0.7°C placebo, P=0.38) or any secondary outcome was found. Pain levels were similar (2.8±1.6 nifedipine vs 3.0±1.5 placebo, P=0.32). The most common adverse event was headache (32% of nifedipine trials vs 8% placebo). CONCLUSIONS: Pretreatment with 30 mg of oral nifedipine twice daily does not affect the CIVD response in healthy individuals under cold stress.

Wilderness & environmental medicine published new progress about calcium channel blockers; cold injury; environmental medicine; prevention and control. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Computed Properties of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reddy, Suryanarayana Challa published the artcileAmlodipine Induced Gum Hypertrophy: A Rare Case Report., Product Details of C17H18N2O6, the main research area is Calcium channel blockers; amlodipine; anticonvulsants; antihypertensive; drug induced gingival overgrowth; immunosuppressive.

BACKGROUND: DIGO or drug-induced gingival overgrowth occurs as a side effect of certain drugs. Until now, the etiology of drug-induced gingival overgrowth is not clearly understood. Among the calcium channel blockers, nifedipine has been shown to be most frequently associated with drug-induced gingival hyperplasia. Amlodipine is a comparatively newer calcium channel blocker that with a longer duration of action and lesser side effects as compared to nifedipine. There are only certain case reports of amlodipine-induced gum hyperplasia. CASE PRESENTATION: We report a case of amlodipine-induced gum hyperplasia in a 66-year-old hypertensive patient taking amlodipine at a dose of 5 mg once a day. There was significant regression of gum hypertrophy after substitution of amlodipine by Losartan. CONCLUSION: Amlodipine is one of the commonly prescribed antihypertensive drugs, and gingival hyperplasia is one overlooked side effect in patients taking amlodipine. Awareness of this potential side effect of amlodipine may be helpful to reduce the anxiety of patients and the cost of diagnostic procedures.

Current drug safety published new progress about Calcium channel blockers; amlodipine; anticonvulsants; antihypertensive; drug induced gingival overgrowth; immunosuppressive. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem