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calcium channel blockers

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https://www.readbyqxmd.com/read/28214378/calcium-signaling-through-l-type-calcium-channels-role-in-pathophysiology-of-spinal-nociceptive-transmission
#1
REVIEW
Olivier Roca-Lapirot, Houda Radwani, Franck Aby, Frédéric Nagy, Marc Landry Pascal Fossat
L-type voltage-gated calcium channels (VGCCs) are ubiquitous channels in the central nervous system. L-type calcium channels (LTCs) are mostly post-synaptic channels regulating neuronal firing and gene expression. They play a role in important physio-pathological processes such as learning and memory, Parkinson's disease, autism and, as recognized more recently, in the pathophysiology of pain processes. Classically, the fundamental role of these channels in cardiovascular functions has limited the use of classical molecules to treat LTC-dependent disorders...
February 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28202361/pre-clinical-evaluation-of-voltage-gated-calcium-channel-blockers-derived-from-the-spider-p-nigriventer-in-glioma-progression
#2
Natália Fontana Nicoletti, Thaís Cristina Erig, Rafael Fernandes Zanin, Marcelo Ricardo Roxo, Nelson Pires Ferreira, Marcus Vinicius Gomez, Fernanda Bueno Morrone, Maria Martha Campos
This study investigated the effects of P/Q- and N-type voltage-gated calcium channel (VGCC) blockers derived from P. nigriventer in glioma progression, by means of in vitro and in vivo experiments. Glioma cells M059J, U-138MG and U-251MG were used to evaluate the antiproliferative effects of P/Q- and N-type VGCC inhibitors PhTx3-3 and Phα1β from P. nigriventer (0.3-100 pM), in comparison to MVIIC and MVIIA from C. magus (0.3-100 pM), respectively. The toxins were also analyzed in a glioma model induced by implantation of GL261 mouse cells...
February 12, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28197715/vacuolar-ion-channels-in-the-liverwort-marchantia-polymorpha-influence-of-ion-channel-inhibitors
#3
Mateusz Koselski, Kazimierz Trebacz, Halina Dziubinska
Potassium-permeable slow activating vacuolar channels (SV) and chloride-permeable channels in the vacuole of the liverwort Marchantia polymorpha were characterized in respect to calcium dependence, selectivity, and pharmacology. The patch-clamp method was used in the study of ion channel activity in the vacuoles from the liverwort Marchantia polymorpha. The whole-vacuole recordings allowed simultaneous observation of two types of currents-predominant slow activated currents recorded at positive voltages and fast activated currents recorded at negative voltages...
February 14, 2017: Planta
https://www.readbyqxmd.com/read/28197288/serum-triglyceride-lowering-effect-of-cilnidipine-in-patients-with-essential-hypertension
#4
Prakash Kumar, Arijit Das, Satish Chandra, Manju Gari, U S P Keshri, Kusum Kumari
BACKGROUND: Many epidemiological studies have established the relationship between hypertension and dyslipidemia. Calcium channel blockers (CCBs) are one of the first-line drugs for newly diagnosed patients with essential hypertension. Cilnidipine as a newer CCB acting by blocking both L- and N-type calcium channels possesses additional beneficial effects apart from lowering blood pressure (BP). The aim of this study was to evaluate the effectiveness of cilnidipine in patients with essential hypertension with borderline dyslipidemia and its effects on lipid profile...
October 2016: Cardiology Research
https://www.readbyqxmd.com/read/28197287/effects-of-cilnidipine-on-heart-rate-and-uric-acid-metabolism-in-patients-with-essential-hypertension
#5
Arijit Das, Prakash Kumar, Abha Kumari, Satish Chandra, Manju Gari, Nidhi Singh, Debleena Dey
BACKGROUND: The relation between hypertension and hyperuricemia has been established by epidemiological studies. Calcium channel blockers are one of the first-line drugs for newly diagnosed patients with essential hypertension. Cilnidipine is a new calcium channel blocker acting by blocking both L- and N-type calcium channels. The aim of this study was to compare the effectiveness of amlodipine and cilnidipine in patients with essential hypertension and their effects on heart rate and serum uric acid levels...
October 2016: Cardiology Research
https://www.readbyqxmd.com/read/28196770/effect-of-low-intensity-cavitation-on-the-isolated-human-thoracic-artery-in%C3%A2-vitro
#6
Algimantas Bubulis, Vida Garalienė, Vytautas Jurėnas, Jonas Navickas, Saulius Giedraitis
Reported here are the results of an experimental study on the response to low-intensity cavitation induced by low-frequency (4-6 W/cm(2), 20 kHz and 32.6 kHz) ultrasound of isolated human arterial samples taken during conventional myocardial revascularization operations. Studies have found that low-frequency ultrasound results in a significant (48%-54%) increase in isometric contraction force and does not depend on the number of exposures (10 or 20) or the time passed since the start of ultrasound (0, 10 and 20 min), but does depend on the frequency and location (internal or external) of the blood vessels for the application of ultrasound...
February 10, 2017: Ultrasound in Medicine & Biology
https://www.readbyqxmd.com/read/28195225/a-novel-bk-channel-targeted-peptide-suppresses-sound-evoked-activity-in-the-mouse-inferior-colliculus
#7
L L Scott, E J Brecht, A Philpo, S Iyer, N S Wu, S J Mihic, R W Aldrich, J Pierce, J P Walton
Large conductance calcium-activated (BK) channels are broadly expressed in neurons and muscle where they modulate cellular activity. Decades of research support an interest in pharmaceutical applications for modulating BK channel function. Here we report a novel BK channel-targeted peptide with functional activity in vitro and in vivo. This 9-amino acid peptide, LS3, has a unique action, suppressing channel gating rather than blocking the pore of heterologously expressed human BK channels. With an IC50 in the high picomolar range, the apparent affinity is higher than known high affinity BK channel toxins...
February 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28194398/sphincter-of-oddi-function-and-risk-factors-for-dysfunction
#8
REVIEW
Elham Afghani, Simon K Lo, Paul S Covington, Brooks D Cash, Stephen J Pandol
The sphincter of Oddi (SO) is a smooth muscle valve regulating the flow of biliary and pancreatic secretions into the duodenum, initially described in 1887 by the Italian anatomist, Ruggero Oddi. SO dysfunction (SOD) is a broad term referring to numerous biliary, pancreatic, and hepatic disorders resulting from spasms, strictures, and relaxation of this valve at inappropriate times. This review brings attention to various factors that may increase the risk of SOD, including but not limited to: cholecystectomy, opiates, and alcohol...
2017: Frontiers in Nutrition
https://www.readbyqxmd.com/read/28194001/enhancing-vta-cav1-3-l-type-ca-2-channel-activity-promotes-cocaine-and-mood-related-behaviors-via-overlapping-ampa-receptor-mechanisms-in-the-nucleus-accumbens
#9
A Martínez-Rivera, J Hao, T F Tropea, T P Giordano, M Kosovsky, R C Rice, A Lee, R L Huganir, J Striessnig, N A Addy, S Han, A M Rajadhyaksha
Genetic factors significantly influence susceptibility for substance abuse and mood disorders. Rodent studies have begun to elucidate a role of Cav1.3 L-type Ca(2+) channels in neuropsychiatric-related behaviors, such as addictive and depressive-like behaviors. Human studies have also linked the CACNA1D gene, which codes for the Cav1.3 protein, with bipolar disorder. However, the neurocircuitry and the molecular mechanisms underlying the role of Cav1.3 in neuropsychiatric phenotypes are not well established...
February 14, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28193357/efficient-and-clean-pre-concentration-of-ultra-trace-calcium-channel-blockers-from-biological-matrices-via-a-hyphenated-procedure-of-two-sequential-dispersive-solid-liquid-phase-microextractions
#10
Maryam Hemmati, Maryam Rajabi, Alireza Asghari
In the present work, we propose a safe, simple, and relatively rapid procedure for the efficient clean-up and pre-concentration of ultra-trace calcium channel blockers (CCBs) from the human plasma and urine samples followed by high performance liquid chromatography-ultraviolet detection. The proposed sample preparation method is a combination of two microextraction methods termed as ultrasound-assisted dispersive micro solid-phase extraction coupled with air-agitated liquid-liquid microextraction based on solidification of a floating organic droplet (UA-dμSPE-AA-LLME-SFO)...
April 1, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28192423/elucidation-of-molecular-kinetic-schemes-from-macroscopic-traces-using-system-identification
#11
Miguel Fribourg, Diomedes E Logothetis, Javier González-Maeso, Stuart C Sealfon, Belén Galocha-Iragüen, Fernando Las-Heras Andrés, Vladimir Brezina
Overall cellular responses to biologically-relevant stimuli are mediated by networks of simpler lower-level processes. Although information about some of these processes can now be obtained by visualizing and recording events at the molecular level, this is still possible only in especially favorable cases. Therefore the development of methods to extract the dynamics and relationships between the different lower-level (microscopic) processes from the overall (macroscopic) response remains a crucial challenge in the understanding of many aspects of physiology...
February 13, 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/28192226/use-of-preventive-medication-in-patients-with-limited-life-expectancy-a-systematic-review
#12
REVIEW
Arjun Poudel, Patsy Yates, Debra Rowett, Lisa M Nissen
CONTEXT: Optimal prescribing in patients with limited life expectancy remains unclear. OBJECTIVES: This study systematically reviews the published literature regarding the use of preventive medication in patients with reduced life expectancy. METHODS: A systematic literature search was conducted using three databases (MEDLINE, EMBASE and CINAHL). Articles published in English from January 1995 to December 2015 were retrieved for analysis to identify peer-reviewed, observational studies assessing use of preventive medications in patients with limited life expectancy...
February 9, 2017: Journal of Pain and Symptom Management
https://www.readbyqxmd.com/read/28192097/effects-of-iron-overload-an-iron-chelator-and-a-t-type-calcium-channel-blocker-on-cardiac-mitochondrial-biogenesis-and-mitochondrial-dynamics-in-thalassemic-mice
#13
Juthamas Khamseekaew, Sirinart Kumfu, Suwakon Wongjaikam, Sasiwan Kerdphoo, Thidarat Jaiwongkam, Somdet Srichairatanakool, Suthat Fucharoen, Siriporn C Chattipakorn, Nipon Chattipakorn
Although cardiac mitochondrial dysfunction is involved in the pathophysiology of iron-overload cardiomyopathy, the precise mechanisms of iron-induced mitochondrial dysfunction, and the roles of the iron chelator deferiprone and the T-type calcium channel blocker efonidipine on cardiac mitochondrial biogenesis in thalassemic mice are still unknown. β-thalassemic (HT) mice were fed with a normal diet (ND) or a high iron-diet (FE) for 90 days. Then, the FE-fed mice were treated with deferiprone (75mg/kg/day) or efonidipine (4mg/kg/day) for 30 days...
February 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28186527/risk-of-breast-cancer-with-long-term-use-of-calcium-channel-blockers-or-angiotensin-converting-enzyme-inhibitors-among-older-women
#14
Marsha A Raebel, Chan Zeng, T Craig Cheetham, David H Smith, Heather Spencer Feigelson, Nikki M Carroll, Kristin Goddard, Heather M Tavel, Denise M Boudreau, Susan Shetterly, Stanley Xu
No abstract text is available yet for this article.
February 15, 2017: American Journal of Epidemiology
https://www.readbyqxmd.com/read/28185965/cav1-2-but-not-cav1-3-l-type-calcium-channel-subtype-mediates-nicotine-induced-conditioned-place-preference-in-miceo
#15
Yudan Liu, Meghan Harding, Jules Dore, Xihua Chen
Nicotine use is one of the most common forms of drug addiction. Although L-type calcium channels (LTCCs) are involved in nicotine addiction, the contribution of the two primary LTCC subtypes (Cav1.2 and 1.3) is unknown. This study aims to determine the contribution of these two LTCC subtypes to nicotine-induced conditioned place preference (CPP) responses by using transgenic mouse models that do not express Cav1.3 (Cav1.3(-/-)) or contain a mutation in the dihydropyridine (DHP) site of the Cav1.2 (Cav1.2DHP(-/-))...
February 6, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28178210/perindopril-induces-tsp-1-expression-in-hypertensive-patients-with-endothelial-dysfunction-in-chronic-treatment
#16
Valentina Buda, Minodora Andor, Lucian Petrescu, Carmen Cristescu, Dana Emilia Baibata, Mirela Voicu, Melania Munteanu, Ioana Citu, Calin Muntean, Octavian Cretu, Mirela Cleopatra Tomescu
Thrombospondin-1 (TSP-1) is a potent endogenous inhibitor of both physiological and pathological angiogenesis, widely studied as a target in drug development for treating cancer. Several studies performed in the cardiovascular field on TSP-1 are contradictory, the role of TSP-1 in the physiopathology of cardiovascular disorders (CVDs) being, for the moment, incompletely understood and may be due to the presence of several domains in its structure which can stimulate many cellular receptors. It has been reported to inhibit NO-mediated signaling and to act on the angiogenesis, tissue perfusion, endothelial cell proliferation, and homeostasis, so we aimed to quantify the effect Perindopril has on TSP-1 plasma levels in hypertensive patients with endothelial dysfunction in comparison with other antihypertensive drugs, such as beta blockers, calcium channel blockers, and diuretics, in a chronic treatment...
February 7, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28176276/maintained-ltp-and-memory-are-lost-by-zn-2-influx-into-dentate-granule-cells-but-not-ca-2-influx
#17
Atsushi Takeda, Haruna Tamano, Marie Hisatsune, Taku Murakami, Hiroyuki Nakada, Hiroaki Fujii
The idea that maintained LTP and memory are lost by either increase in intracellular Zn(2+) in dentate granule cells or increase in intracellular Ca(2+) was examined to clarify significance of the increases induced by excess synapse excitation. Both maintained LTP and space memory were impaired by injection of high K(+) into the dentate gyrus, but rescued by co-injection of CaEDTA, which blocked high K(+)-induced increase in intracellular Zn(2+) but not high K(+)-induced increase in intracellular Ca(2+). High K(+)-induced disturbances of LTP and intracellular Zn(2+) are rescued by co-injection of 6-cyano-7-nitroquinoxakine-2,3-dione, an α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonist, but not by co-injection of blockers of NMDA receptors, metabotropic glutamate receptors, and voltage-dependent calcium channels...
February 7, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28174958/p029-azelnidipine-a-novel-calcium-channel-blocker-ameliorates-severity-of-colitis-in-dss-induced-colitis-in-mice-possibly-by-modulating-tissue-levels-of-tnf-alpha-and-il-6
#18
T Kav, A Akyol, E Aksoy, C Ozer, M Torgutalp, B Sivri
No abstract text is available yet for this article.
February 1, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28168659/btp2-a-store-operated-calcium-channel-inhibitor-attenuates-lung-ischemia-reperfusion-injury-in-rats
#19
Wei Zhang, Zeyou Qi, Yaping Wang
Lung ischemia-reperfusion (I/R) injury is a critical complication following a lung transplant, cardiopulmonary bypass, pulmonary embolism, and trauma. Immune cells and their effector functions are involved in the lung I/R injury. Store-operated calcium channels (SOCC) are highly Ca(2+)-selective cation channels and have crucial effects on the immune system. It has been indicated that BTP2, a potent SOCC blocker, could inhibit pro-inflammatory cytokine production from immune cells both in vitro and in vivo. Therefore, this study was conducted to investigate the beneficial effects of BTP2 on lung I/R injury in Sprague-Dawley (SD) rats...
February 7, 2017: Inflammation
https://www.readbyqxmd.com/read/28163539/inhibition-by-tadalafil-of-contractility-of-isolated-nonpregnant-human-myometrium
#20
Sumalya Sen, Anitha Thomas, Saibal Das, Jayanta Kumar Dey, Abraham Peedicayil, Vinotha Thomas, Jacob Peedicayil
OBJECTIVE: To investigate the inhibitory effect of tadalafil on the contractility of isolated nonpregnant human myometrium. MATERIALS AND METHODS: The ability of tadalafil (25, 40, and 63 μM) to inhibit 55 mM KCl-induced contractility of isolated nonpregnant human myometrium was studied. The ability of the ATP-sensitive potassium channel blocker glibenclamide (10 μM) and the calcium-sensitive potassium channel (BKCa) blocker iberiotoxin (100 nM) to reverse the inhibitory effect of 40 μM tadalafil on 55 mM KCl-induced myometrial contractility was also studied...
October 2016: Journal of Pharmacology & Pharmacotherapeutics
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