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Specialty: Drugs & Pharmacology
Nutrition: Calcium

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Total 116 results found since Jan 2013.

Endothelial Small- and Intermediate-Conductance K Channels and Endothelium-Dependent Hyperpolarization as Drug Targets in Cardiovascular Disease.
Abstract Endothelial calcium/calmodulin-gated K channels of small (KCa2.3) and intermediate conductance (KCa3.1) produce membrane hyperpolarization and endothelium-dependent hyperpolarization (EDH)-mediated vasodilation. Dysfunctions of the two channels and ensuing EDH impairments are found in several cardiovascular pathologies such as diabetes, atherosclerosis, postangioplastic neointima formation, but also inflammatory disease, cancer, and organ fibrosis. Moreover, KCa3.1 plays an important role in endothelial barrier dysfunction, edema formation in cardiac and pulmonary disease, and in ischemic stroke. Concerni...
Source: Advances in Pharmacology - July 29, 2016 Category: Drugs & Pharmacology Authors: Köhler R, Oliván-Viguera A, Wulff H Tags: Adv Pharmacol Source Type: research

Neuroprotection of taurine against reactive oxygen species is associated with inhibiting NADPH oxidases.
Abstract It is well established that taurine shows potent protection against glutamate-induced injury to neurons in stroke. The neuroprotection may result from multiple mechanisms. Increasing evidences suggest that NADPH oxidases (Nox), the primary source of superoxide induced by N-methyl-d-aspartate (NMDA) receptor activation, are involved in the process of oxidative stress. We found that 100μM NMDA induced oxidative stress by increasing the reactive oxygen species level, which contributed to the cell death, in vitro. Neuron cultures pretreated with 25mM taurine showed lower percentage of death cells and decline...
Source: European Journal of Pharmacology - March 2, 2016 Category: Drugs & Pharmacology Authors: Han Z, Gao LY, Lin YH, Chang L, Wu HY, Luo CX, Zhu DY Tags: Eur J Pharmacol Source Type: research

Atherosclerotic cardiovascular disease: a review of initiators and protective factors
Abstract Atherosclerotic cardiovascular disease (CVD) is a collective term comprising of a group of disorders of the heart and blood vessels. These diseases are the largest cause of morbidity and premature death worldwide. Coronary heart disease and cerebrovascular disease (stroke) are the most frequently occurring diseases. The two major initiators involved in the development of atherosclerotic CVD are vascular production of reactive oxygen species (ROS) and lipid oxidation. In atherosclerosis development, ROS is associated with rapid loss of anti-inflammatory and anti-atherogenic activities of the endothelium-de...
Source: Inflammopharmacology - January 11, 2016 Category: Drugs & Pharmacology Source Type: research

The neuroprotective effects of R-phenibut after focal cerebral ischemia
In this study, MCAO was induced by filament insertion (f-MCAO) or endothelin-1 (ET1) microinjection (ET1-MCAO) in Male Wistar or CD rats, respectively. R-phenibut was administrated at doses of 10 and 50mg/kg for 14 days in the f-MCAO or 7 days in the ET1-MCAO. The vibrissae-evoked forelimb-placing and limb-placing tests were used to assess sensorimotor, tactile and proprioceptive function. Quantitative real time-PCR was used to detect brain-derived neurotrophic factor (BDNF) and vascular endothelial growth factor (VEGF) gene expression in the damaged brain hemisphere.Both f-MCAO and ET1-MCAO resulted in statistically signi...
Source: Pharmacological Research - November 25, 2015 Category: Drugs & Pharmacology Source Type: research

Visit-to-visit blood pressure variability and classes of antihypertensive agents; associations with artery remodeling and the risk of stroke.
Abstract Recent studies have shown that visit-to-visit blood pressure (BP) variability was emerging as an independent risk factor for stroke. Although the mechanism is not fully understood, artery remodeling would be closely associated with the relationship between visit-to-visit BP variability and stroke. In addition, the class of antihypertensive agents is suggested to be an important determinant of visit-to-visit BP variability. This review article summarizes the recent literature on these topics. In the elderly hypertensives, strict BP control using calcium channel blockade would play a crucial role to prevent...
Source: Current Pharmaceutical Design - November 12, 2015 Category: Drugs & Pharmacology Authors: Nagai M, Dote K, Kato M, Sasaki S, Oda N, Kagawa E, Nakano Y, Yamane A, Kubo Y, Higashihara T, Miyauchi S, Harada W Tags: Curr Pharm Des Source Type: research

A Systematic Review on the Efficacy of Amlodipine in the Treatment of Patients With Hypertension With Concomitant Diabetes Mellitus and/or Renal Dysfunction, When Compared With Other Classes of Antihypertensive Medication
The long-term cardiovascular (CV) effects of calcium channel blockers, with special focus on amlodipine, were compared with other classes of antihypertensive medications in high-risk hypertensive patient subgroups. A systematic literature review and meta-analysis was undertaken of 38 unique randomized, active-controlled, parallel-group trials comparing amlodipine/calcium channel blockers with diuretics, β-blockers, α-blockers, angiotensin-converting enzyme inhibitors, or angiotensin II receptor blockers, with ≥6-month follow-up, and which had included assessment of blood pressure (BP) and CV events [all-cause death, CV...
Source: American Journal of Therapeutics - September 1, 2015 Category: Drugs & Pharmacology Tags: Original Articles Source Type: research

Connexin 43 stabilizes astrocytes in a stroke-like milieu to facilitate neuronal recovery
yin Feng
Source: Acta Pharmacologica Sinica - August 4, 2015 Category: Drugs & Pharmacology Authors: Le-yu WuXue-li YuLin-yin Feng Tags: astrocytes Connexin 43 oxygen-glucose deprivation/recovery middle cerebral artery occlusion CREB Ephrin-A4 calcium Source Type: research

Neuroprotective peptides fused to arginine-rich cell penetrating peptides: Neuroprotective mechanism likely mediated by peptide endocytic properties
In conclusion, we believe that there are strong grounds to regard arginine-rich peptides as a new class of neuroprotective molecules for the treatment of a range neurological disorders.
Source: Pharmacology and Therapeutics - June 26, 2015 Category: Drugs & Pharmacology Source Type: research

Poly(ADP-ribose)polymerase 1 (PARP-1) activation and Ca2+ permeable α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) channels in post-ischemic brain damage: new therapeutic opportunities?
Abstract A significant number of laboratories observed that poly (ADP-ribose) polymerase (PARP) inhibitors, administered a few hours after ischemic or traumatic brain injury, may drastically reduce the subsequent neurological damage. It has also been shown that PARP inhibitors, administered for 24 hours to rats with permanent middle cerebral artery occlusion (MCAO), may reduce the number of dying neurons for a long period after surgery, thus suggesting that these agents could reduce the delayed brain damage and the neurological and cognitive impairment (dementia) frequently observed a few months after a stroke. In...
Source: CNS and Neurological Disorders Drug Targets - April 30, 2015 Category: Drugs & Pharmacology Authors: Gerace E, Pellegrini-Giampietro DE, Moroni F, Mannaioni G Tags: CNS Neurol Disord Drug Targets Source Type: research

Towards Understanding the Role of the Na(+)-Ca (2+) Exchanger Isoform 3.
Abstract The Na(+)-Ca(2+) exchanger (NCX) is critical for Ca(2+) homeostasis throughout the body. Of the three isoforms in the NCX family, NCX1 has been extensively studied, providing a good basis for understanding the molecular aspects of the NCX family, including structural resemblances, stoichiometry, and mechanism of exchange. However, the tissue expression of the third isoform of the family, NCX3, together with its proposed involvement in the Ca(2+) fluxes of the endoplasmic reticulum and the mitochondria suggests a distinctive role for this isoform. Investigations of the exchanger revealed the involvement of...
Source: Pharmacological Reviews - April 8, 2015 Category: Drugs & Pharmacology Authors: Michel LY, Hoenderop JG, Bindels RJ Tags: Rev Physiol Biochem Pharmacol Source Type: research

Rapamycin ameliorates brain metabolites alterations after transient focal ischemia in rats.
In this study, the neuroprotective effect of rapamycin on the metabolic changes induced by MCAo was evaluated using nuclear magnetic resonance (NMR) spectroscopy of brain tissues. MCAo in rats was induced by insertion of nylon filament. One hour after ischemia, rapamycin (250µg/kg,i.p.) in dimethyl sulfoxide was administered. Reperfusion was done 2h after ischemia. Twenty-four hours after ischemia phospholipase A2 (PLA2) levels and metabolic changes were assessed. Perchloric acid extraction was performed on the brain of all animals (n=7; sham, vehicle; DMSO and rapamycin 250µg/kg) and the various brain metabolites were a...
Source: European Journal of Pharmacology - March 23, 2015 Category: Drugs & Pharmacology Authors: Chauhan A, Sharma U, Jagannathan NR, Gupta YK Tags: Eur J Pharmacol Source Type: research

Drug Therapy of Apparent Treatment-Resistant Hypertension: Focus on Mineralocorticoid Receptor Antagonists
Abstract Apparent treatment-resistant hypertension (aTRH) is defined as blood pressure (BP) >140/90 mmHg despite three different antihypertensive drugs including a diuretic. aTRH is associated with an increased risk of cardiovascular events, including stroke, chronic renal failure, myocardial infarction, congestive heart failure, aortic aneurysm, atrial fibrillation, and sudden death. Preliminary studies of renal nerve ablation as a therapy to control aTRH were encouraging. However, these results were not confirmed by the Symplicity 3 trial. Therefore, attention has refocused on drug therapy. Secondary forms o...
Source: Drugs - March 19, 2015 Category: Drugs & Pharmacology Source Type: research

The involvement of the sigma-1 receptor in neurodegeneration and neurorestoration
Publication date: Available online 9 December 2014 Source:Journal of Pharmacological Sciences Author(s): Karsten Ruscher , Tadeusz Wieloch The Sigma-1 receptor (Sig-1R) is a single 25 kD polypeptide and a chaperone protein immersed in lipid rafts of the endoplasmic reticulum (ER) where it interacts with mitochondria at the mitochondria-associated ER membrane domain (MAM). Upon activation, the Sig-1R binds to the inositol trisphosphate receptor (IP3R), and modulates cellular calcium (Ca2+) homeostasis. Also, the activated Sig-1R modulates plasma membrane receptor and ion channel functions, and may regulate cellular excita...
Source: Journal of Pharmacological Sciences - December 11, 2014 Category: Drugs & Pharmacology Source Type: research

Bedtime Hypertension Chronotherapy: Concepts and Patient Outcomes.
Abstract Recent findings indicate cardiovascular disease (CVD) risk is best predicted by asleep systolic blood pressure (SBP), and lowering it by scheduling ≥1 conventional long-acting hypertension medications, alone or in combination, at bedtime significantly lessens vascular-associated risks. Some 20 years ago, four controlled-onset extended-release drug-delivery systems incorporating a calcium channel blocker or β-blocker, with the treatment goal specifically being attenuation of morning rather than asleep BP, were conceived as one type of bedtime hypertension chronotherapy. However, the CONVINCE outcomes tr...
Source: Current Pharmaceutical Design - October 24, 2014 Category: Drugs & Pharmacology Authors: Smolensky MH, Hermida RC, Ayala DE, Portaluppi F Tags: Curr Pharm Des Source Type: research

Drug delivery to the ischemic brain.
Abstract Cerebral ischemia occurs when blood flow to the brain is insufficient to meet metabolic demand. This can result from cerebral artery occlusion that interrupts blood flow, limits CNS supply of oxygen and glucose, and causes an infarction/ischemic stroke. Ischemia initiates a cascade of molecular events in neurons and cerebrovascular endothelial cells including energy depletion, dissipation of ion gradients, calcium overload, excitotoxicity, oxidative stress, and accumulation of ions and fluid. Blood-brain barrier (BBB) disruption is associated with cerebral ischemia and leads to vasogenic edema, a primary ...
Source: Advances in Pharmacology - October 15, 2014 Category: Drugs & Pharmacology Authors: Thompson BJ, Ronaldson PT Tags: Adv Pharmacol Source Type: research