Month: December 2022

Suzuki, Yoshiaki published the artcileLocal Ca2+ Signals within Caveolae Cause Nuclear Translocation of CaMK1α in Mouse Vascular Smooth Muscle Cells., SDS of cas: 21829-25-4, the main research area is Ca2+/calmodulin-dependent kinase; L-type Ca2+ channel; caveola; fluorescence imaging; vascular smooth muscle cell.

An increase in intracellular Ca2+ concentration ([Ca2+]i) activates Ca2+-sensitive enzymes such as Ca2+/calmodulin-dependent kinases (CaMK) and induces gene transcription in various types of cells. This signaling pathway is called excitation-transcription (E-T) coupling. Recently, we have revealed that a L-type Ca2+ channel/CaMK kinase (CaMKK) 2/CaMK1α complex located within caveolae in vascular smooth muscle cells (SMCs) can convert [Ca2+]i changes to gene transcription profiles that are related to chemotaxis. Although CaMK1α is expected to be the key molecular identity that can transport Ca2+ signals originated within caveolae to the nucleus, data sets directly proving this scheme are lacking. In this study, multicolor fluorescence imaging methods were utilized to address this question. Live cell imaging using mouse primary aortic SMCs revealed that CaMK1α can translocate from the cytosol to the nucleus; and that this movement was blocked by nifedipine or a CaMKK inhibitor, STO609. Experiments using two types of Ca2+ chelators, ethylene glycol-bis(2-aminoethylether)-N,N,N’,N’-tetraacetic acid (EGTA) and 1,2-bis(2-aminophenoxy)ethane-N,N,N’,N’-tetraacetic acid (BAPTA), combined with caveolin-1 knockout (cav1-KO) mice showed that local Ca2+ events within caveolae are required to trigger this CaMK1α nuclear translocation. Importantly, overexpression of cav1 in isolated cav1-KO myocytes recovered the CaMK1α translocation. In SMCs freshly isolated from mesenteric arteries, CaMK1α was localized mainly within caveolae in the resting state. Membrane depolarization induced both nuclear translocation and phosphorylation of CaMK1α. These responses were inhibited by nifedipine, STO609, cav1-KO, or BAPTA. These new findings strongly suggest that CaMK1α can transduce Ca2+ signaling generated within or very near caveolae to the nucleus and thus, promote E-T coupling.

Biological & pharmaceutical bulletin published new progress about Ca2+/calmodulin-dependent kinase; L-type Ca2+ channel; caveola; fluorescence imaging; vascular smooth muscle cell. 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, SDS of cas: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rivera-Gonzalez, Jonatahan published the artcileUse of Sublingual Nitrates for Management of Limb Ischemia Secondary to Inadvertent Intra-Arterial Buprenorphine/Naloxone (Suboxone®) Film Injection., Related Products of pyridine-derivatives, the main research area is Buprenorphine; Intravenous drug user; Limb ischemia; Naloxone; Nitroglycerine; Suboxone.

Multiple case reports have signaled a rise in buprenorphine abuse in the US, particularly among inmates. We present the case of limb ischemia secondary to accidental intra-arterial buprenorphine/naloxone film injection successfully treated with sublingual nitroglycerin. A 39-year-old man with history of intravenous drug use presented sudden severe left hand pain since three days prior to evaluation. Pain was preceded by self-injection of dissolved buprenorphine/naloxone sublingual film onto the affected arm. An arteriogram suggested severe vasoconstriction in the absence of frank thrombosis. Patient was initially treated with continuous heparin infusion and nifedipine. Forty-eight hours later, due to poor response, sublingual nitroglycerin was added to therapy. Digits regained color, sensation, and pain resolved within 15 minutes of administration of sublingual nitroglycerin. The presence of acute limb ischemia caused by prolonged vasospasm is a very rare complication. A normal angiogram should raise suspicion regarding vasospasm as the mechanism of ischemia, and prompt nitroglycerin therapy.

Puerto Rico health sciences journal published new progress about Buprenorphine; Intravenous drug user; Limb ischemia; Naloxone; Nitroglycerine; Suboxone. 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, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Morimoto, Kohkichi published the artcileBullous pemphigoid in patients receiving peritoneal dialysis: a case series and a literature survey., Formula: C17H18N2O6, the main research area is Bullous pemphigoid; hemodialysis; incidence; peritoneal dialysis.

Bullous pemphigoid (BP) is an autoimmune subepidermal blistering disease. Although several cases of BP in end-stage renal disease patients receiving peritoneal dialysis (PD) or hemodialysis have been reported, the incidence of BP in these patients remains unknown. We recently experienced three PD patients diagnosed with BP. The skin injury was likely to be a trigger of BP in all the three PD patients. Nifedipine and icodextrin exposures were possible factors directly or indirectly affecting the onset of BP, because they were common in the three cases. We also report that the incidence of BP in PD patients was 3/478.3 person-years in a single-center 10-year study. This case series with a literature survey describes that the skin and tissue injuries are potential triggers responsible for the onset of BP in dialysis patients and that the incidence of BP in these patients seems to be much higher than that in the general population.

Renal failure published new progress about Bullous pemphigoid; hemodialysis; incidence; peritoneal dialysis. 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, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Van der Lans, H. N. M. published the artcileDidehydrohetarenes. XXIII. Does 2,6-didehydropyridine exist, Recommanded Product: 2-Bromo-4-ethoxypyridine, the main research area is bromo aminopyridine piperidide; bromo aminoquinoline piperidide; pyridines bromo piperidide; quinoline bromo piperidide; didehydropyridine existence.

3-Amino-2-bromopyridine with Li piperidide gave pyrrole-3-carbonitrile; 4-amino-2-bromopyridine gave a ring-opened product (I); 5-amino-2-bromopyridine gave II and III; 6-amino-2-bromopyridine gave IV. 4-Amino-2-bromoquinoline gave V and VI. The intermediacy of 2,6-didehydropyridine in these reactions was discussed.

Tetrahedron Letters published new progress about bromo aminopyridine piperidide; bromo aminoquinoline piperidide; pyridines bromo piperidide; quinoline bromo piperidide; didehydropyridine existence. 17117-13-4 belongs to class pyridine-derivatives, name is 2-Bromo-4-ethoxypyridine, and the molecular formula is C7H8BrNO, Recommanded Product: 2-Bromo-4-ethoxypyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Di Stefano, Vincenzo published the artcileTumour-like presentation of atypical posterior reversible encephalopathy syndrome with prominent brainstem involvement., Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Brain stem/cerebellum; neuro-oncology; neuroimaging; neurology; radiology.

Typical posterior reversible encephalopathy syndrome (PRES) is a clinical-neuroradiological entity characterised by bilateral white matter oedema, which is usually symmetrical and totally reversible in 2-3 weeks. A 46-year-old man presented with a persistent headache and visual blurring in the right eye. On admission, the clinical examination revealed minimal unsteadiness of gait and elevated blood pressure. A brain MRI showed a hyperintense signal on T2-weighted sequences in the whole brainstem, extended to the spinal cord (C2-C6), the left insula and the right cerebellum. When his blood pressure was controlled, his symptoms gradually improved. The follow-up MRI scan at 3 weeks revealed a dramatic regression of the hyperintense lesions on T2-weighted sequences. The differential diagnosis of PRES is very wide, especially in the case of conspicuous brainstem involvement. Treatable causes of white matter oedema should be always kept in mind to avoid misdiagnosis and prevent complications, such as intracranial haemorrhage.

BMJ case reports published new progress about Brain stem/cerebellum; neuro-oncology; neuroimaging; neurology; radiology. 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Xuena published the artcileBradyarrhythmia and hypotension during anesthetic induction-reconsideration of nifedipine: a case report., Quality Control of 21829-25-4, the main research area is Bradyarrhythmia; advanced age; anesthesia; case report; hypotension; nifedipine.

Cardiac events sometimes occur during anesthesia and surgery and may be severe or even life-threatening. This report describes a case of severe bradyarrhythmia during anesthetic induction with propofol, midazolam, sufentanil, and vecuronium. The patient took nifedipine sustained-release tablets on the morning of surgery as routine treatment for hypertension, and this medication may have contributed to the bradyarrhythmia. Nifedipine is a calcium channel blocker that can dilate blood vessels, depress the activity of the sinoatrial node, and delay the conduction of the atrioventricular node. Although these effects are not usually significant, they may be enhanced by anesthetics or other concomitant drugs. For patients of advanced age, especially those with autonomic disturbance or cardiac abnormalities, these effects can be remarkable, and discontinuation of nifedipine should be considered.

The Journal of international medical research published new progress about Bradyarrhythmia; advanced age; anesthesia; case report; hypotension; 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, Quality Control of 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xu, Qian published the artcileCost-effectiveness analysis of combining traditional Chinese medicine in the treatment of hypertension: compound Apocynum tablets combined with Nifedipine sustained-release tablets vs Nifedipine sustained-release tablets alone., Category: pyridine-derivatives, the main research area is Blood pressure variability; Compound Apocynum tablets; Cost-effectiveness analysis; Markov model; Nifedipine sustained-release tablets; TCMs.

BACKGROUND: We evaluated the long-term cost-effectiveness of antihypertensive traditional Chinese medicines (TCMs) and to compare the cost-effectiveness of a combined treatment consisting of compound Apocynum tablets and Nifedipine sustained-release tablets with the cost-effectiveness of treatment with Nifedipine sustained-release tablets alone. METHODS: A Markov model was used to simulate the potential incremental cost-effectiveness per quality-adjusted life year (QALY) to be gained from compound Apocynum tablets and Nifedipine sustained-release tablets compared with Nifedipine sustained-release tablets alone. Model parameter estimates were informed by previously published studies. The direct medical costs of outpatients with hypertension were estimated from the health care provider’s perspective. A 5% annual discount rate was applied to both costs and QALYs. RESULTS: TCMs combined with Nifedipine sustained-release tablets group generated a total 20-year cost of 11,517.94 RMB (US $1739.87), whereas Nifedipine sustained-release tablets alone group resulted in a 20-year cost of 7253.71 RMB (US $1095.73). TCMs combined with Nifedipine sustained-release tablets group resulted in a generation of 12.69 QALYs, whereas Nifedipine sustained-release tablets alone group resulted in 12.50. The incremental cost-utility ratio was 22,443.32 RMB (US $3390.23) per QALY. Considering the threshold of 1 GDP per capita in China in 2018 (US $9764.95), the combination of compound Apocynum tablets and Nifedipine sustained-release tablets was a cost-effective strategy. One-way and probabilistic sensitivity analysis showed unchanged results over an acceptable range. CONCLUSIONS: Combining Traditional Chinese Medicines with chemical medicines is more cost-effective strategy in the treatment of hypertension.

BMC complementary medicine and therapies published new progress about Blood pressure variability; Compound Apocynum tablets; Cost-effectiveness analysis; Markov model; Nifedipine sustained-release tablets; TCMs. 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

Park, Ji-won published the artcileRole of kaempferol to increase bioavailability and pharmacokinetics of nifedipine in rats, Formula: C17H18N2O6, the main research area is Bioavailability; CYP3A4; Kaempferol; Nifedipine; P-gp; Pharmacokinetics.

Herein, the purpose of this study is to evaluate the effects of kaempferol on bioavailability and pharmacokinetics of nifedipine and its metabolite dehydronifedipine in rats. The exptl. design is based on with or without kaempferol in the oral and i.v. administration of nifedipine in rats. Moreover, the pharmacokinetic parameters including nifedipine and dehydronifedipine were evaluated in rats. The in vitro studies of kaempferol were investigated on P-glycoprotein (P-gp) and cytochrome P 450 (CYP) 3A4 activity. Kaempferol reduced a 50% inhibitory concentration (IC50) of 8.6 μmol·L-1 on CYP3A4 enzyme activity. Moreover, kaempferol clearly improved the cell internalization of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp. Depending on increased concentrations of kaempferol, the areas under the plasma concentration-time curve (AUC0-âˆ? and the peak concentration (Cmax) of nifedipine were increased after oral and i.v. administration. Moreover, the absolute bioavailability (AB) and relative bioavailability (RB) of nifedipine in the presence of kaempferol was significantly higher than those of the control group after oral and i.v. administration. Improvement of bioavailability of nifedipine by kaempferol may be mainly because of the inhibition of the P-gp-mediated efflux transporter in the small intestine and CYP3A4-mediated metabolism in the small intestine or liver, or both.

Chinese Journal of Natural Medicines (Amsterdam, Netherlands) published new progress about Bioavailability; CYP3A4; Kaempferol; Nifedipine; P-gp; Pharmacokinetics. 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, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhou, Like published the artcileElucidation on inhibition and binding mechanism of bovine liver catalase by nifedipine: multispectroscopic analysis and computer simulation methods, HPLC of Formula: 21829-25-4, the main research area is binding mode; bovine liver catalase; computer simulation; nifedipine; spectroscopy.

Nifedipine (NDP), a dihydropyridine calcium antagonist, is widely used for the treatment of hypertension and angina pectoris. Catalase is a key antioxidant enzyme that is closely relevant to the level of reactive oxygen specie in vivo. Here, the research explored the effects of NDP on the conformation and catalytic function of bovine liver catalase (BLC) through enzymic reaction kinetic techniques, multispectroscopic anal., and computer simulation methods. Kinetic studies clarified that the NDP reduced the activity of BLC using a noncompetitive inhibition mechanism. Based on trial data, a static quenching mechanism functioned in quenching the intrinsic fluorescence of BLC. The binding constant value was (4.486 ± 0.008) x 104 M-1 (298 K) and BLC had one binding site for NDP. Tyr was prone to be exposed more to a hydrophilic environment in wake of a shift in fluorescence value. The binding reaction of BLC to NDP caused a conformational change in BLC, which in turn led to increase in the α-helix content and a decline in the β-sheet content. Furthermore, several amino acids residues interacted with NDP by means of van der Waals forces, whereas Gln397, Asn368, Gln371, Asn384, and Pro377 formed several hydrogen bonds with NDP.

Luminescence published new progress about binding mode; bovine liver catalase; computer simulation; nifedipine; 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, HPLC of Formula: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Acharya, Aviseka published the artcileParabolic, flight-induced, acute hypergravity and microgravity effects on the beating rate of human cardiomyocytes, Computed Properties of 21829-25-4, the main research area is Bay-K8644; Isoprenaline; L-type Ca2+ channels; adrenoceptor agonist; cardiomyocytes; human induced pluripotent stem cells; hypergravity; microgravity.

Functional studies of human induced pluripotent stem cell (hiPSC)-derived cardiomyocytes (hCMs) under different gravity conditions contribute to aerospace medical research. To study the effects of altered gravity on hCMs, we exposed them to acute hypergravity and microgravity phases in the presence and absence of the β-adrenoceptor isoprenalin (ISO), L-type Ca2+ channel (LTCC) agonist Bay-K8644, or LTCC blocker nifedipine, and monitored their beating rate (BR). These logistically demanding experiments were executed during the 66th Parabolic Flight Campaign of the European Space Agency. The hCM cultures were exposed to 31 alternating hypergravity, microgravity, and hypergravity phases, each lasting 20-22 s. During the parabolic flight experiment, BR and cell viability were monitored using the xCELLigence real-time cell analyzer Cardio Instrument Corresponding experiments were performed on the ground (1 g), using an identical set-up. Our results showed that BR continuously increased during the parabolic flight, reaching a 40% maximal increase after 15 parabolas, compared with the pre-parabolic (1 g) phase. However, in the presence of the LTCC blocker nifedipine, no change in BR was observed, even after 31 parabolas. We surmise that the parabola-mediated increase in BR was induced by the LTCC blocker. Moreover, the increase in BR induced by ISO and Bay-K8644 during the pre-parabola phase was further elevated by 20% after 25 parabolas. This addnl. effect reflects the pos. impact of the parabolas in the absence of both agonists. Our study suggests that acute alterations of gravity significantly increase the BR of hCMs via the LTCC.

Cells published new progress about Bay-K8644; Isoprenaline; L-type Ca2+ channels; adrenoceptor agonist; cardiomyocytes; human induced pluripotent stem cells; hypergravity; microgravity. 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