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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/28212471/-management-of-ureteric-colic-with-ketorolac-and-nifedipin-vs-ketorolac-and-tamsulosin-in-the-emergency-room
#2
Álvaro J Montiel-Jarquín, Valeria M Rocha-Rocha, Hugo A Solís-Mendoza, María S Romero-Figueroa, Ivet Etchegaray-Morales, Ivan Alvarado-Ortega
BACKGROUND: Ureteric colic is the most common symptom of lithiasis. It is caused by the presence of stones accumulated in the renal papillae. These stones often migrate down the ureter, causing a ureteric colic, characterized by a severe pain in the lumbar region. The aim of this study was to compare the use of ketorolac and nifedipine vs. ketorolac and tamsulosin for the medical treatment of pain caused by stones in the lower ureter. METHODS: Longitudinal study of 150 patients of 21-years or older with stones in the lower third of the ureter...
2017: Revista Médica del Instituto Mexicano del Seguro Social
https://www.readbyqxmd.com/read/28209036/-primary-culture-and-functional-identification-of-distal-pulmonary-artery-smooth-muscle-cells-in-mice
#3
M C Li, Y Q Chen, C T Zhang, Q Jiang, W J Lu, J Wang
Objective: To establish a method of isolation and primary culture of mice distal pulmonary artery smooth muscle cells (PASMCs) and identify the functional properties. Methods: PASMCs were harvested from the distal pulmonary artery (PA) tissue of mice by enzymatic digestion of collagenaseⅠand papain; and the growth characteristics were observed under inverted microscope and identified by Immunofluorescence technique. Effects on the intracellular calcium ion concentration of distal PASMCs were detected by Fura-2-AM fluorescent probe tracer under a fluorescence microscope in Krebs solution containing clopiazonic acid (CPA) and nifedipin (Nif)...
February 12, 2017: Chinese Journal of Tuberculosis and Respiratory Diseases
https://www.readbyqxmd.com/read/28203390/soluble-vascular-cell-adhesion-molecule-1-and-magnesium-sulfate-with-nifedipine-treatment-in-indonesian-women-with-severe-pre-eclampsia
#4
REVIEW
Hotma Partogi Pasaribu, Herman Hariman, R Haryono Roeshadi, Stephen C L Koh
BACKGROUND: Endothelial cell activation in pre-eclampsia is associated with elevated soluble vascular cell adhesion molecule-1 (sVCAM-1) levels. The objective of the study was to determine whether sVCAM-1 levels in Indonesian women with pre-eclampsia were similar to other ethnic studies and to determine the effects of magnesium sulfate with nifedipine on blood pressure. METHODS: A total of 61 pregnant women were admitted, who had normal pregnancy (n = 25) and severe pre-eclampsia (n = 36)...
September 2016: Interventional Medicine & Applied Science
https://www.readbyqxmd.com/read/28202717/%C3%AE-adrenoceptor-activation-enhances-l-type-calcium-channel-currents-in-anterior-piriform-cortex-pyramidal-cells-of-neonatal-mice-implication-for-odor-learning
#5
Abhinaba Ghosh, Bandhan Mukherjee, Xihua Chen, Qi Yuan
Early odor preference learning occurs in one-week-old rodents when a novel odor is paired with a tactile stimulation mimicking maternal care. β-Adrenoceptors and L-type calcium channels (LTCCs) in the anterior piriform cortex (aPC) are critically involved in this learning. However, whether β-adrenoceptors interact directly with LTCCs in aPC pyramidal cells is unknown. Here we show that pyramidal cells expressed significant LTCC currents that declined with age. β-Adrenoceptor activation via isoproterenol age-dependently enhanced LTCC currents...
March 2017: Learning & Memory
https://www.readbyqxmd.com/read/28201961/development-and-characterization-pulsatile-microspheres-of-nifedipine-for-hypertension
#6
Rahul Taneja, Ghanshyam Das Gupta
AIM AND BACKGROUND: To develop pulsatile microspheres of Nifedipine blend of polymers Carbopol 971P and Eudragit RS100 for antihypertensive to release the drug at a particular lag time. METHODS: Pulsatile nifedipine microspheres were prepared using blend of Carbopol 971P and Eudragit RS100 at different ratio in a mixture of solvents. Formulations were prepared and optimized on the basis of particle size, percentage yield and drug entrapment efficiency. Optimized formulations were further analyzed at different resolutions per minute (rpm) by optical microscopy, scanning electron microscopy (SEM), in-vitro dissolution studies and kinetics model...
February 12, 2017: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/28196829/marmoset-cytochrome-p450-3a4-expressed-in-liver-and-small-intestine-tissues-efficiently-metabolizes-midazolam-alprazolam-nifedipine-and-testosterone
#7
Shotaro Uehara, Yasuhiro Uno, Kazuyuki Nakanishi, Sakura Ishii, Takashi Inoue, Erika Sasaki, Hiroshi Yamazaki
Common marmosets (Callithrix jacchus), small New World primates, are increasingly attracting attention as potentially useful animal models for drug development. However, characterization of cytochrome P450 (P450) 3A enzymes involved in the metabolism of a wide variety of drugs has remained in marmosets. In this study, sequence homology, tissue distribution, and enzymatic property of marmoset P450 3A4 orthologue, 3A5 orthologue, and 3A90 were investigated. Marmoset P450 3A forms exhibited high amino acid sequence identities (88-90%) to the human and cynomolgus monkey P450 3A orthologues and evolutionary closeness to human and cynomolgus monkey P450 3A orthologues, compared with other P450 3A enzymes...
February 14, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28193694/different-cav1-3-channel-isoforms-control-distinct-components-of-the-synaptic-vesicle-cycle-in-auditory-inner-hair-cells
#8
Philippe Fy Vincent, Yohan Bouleau, Gilles Charpentier, Alice Emptoz, Saaid Safieddine, Christine Petit, Didier Dulon
The mechanisms orchestrating transient and sustained exocytosis in auditory inner hair cells (IHCs) remain largely unknown. These exocytotic responses are believed to mobilize sequentially a readily releasable pool of vesicles (RRP) underneath the synaptic ribbons and a slowly releasable pool of vesicles (SRP) at farther distance from them. They are both governed by Cav1.3 channels and require otoferlin as Ca(2+) sensor but whether they use the same Cav1.3 isoforms is still unknown. Using whole cell patch clamp recordings in post-hearing mice, we show that only a proportion (∼25 %) of the total Ca(2+) current in IHCs, displaying fast inactivation and resistance to 20 μM nifedipine, a L-type Ca(2+) channel blocker, is sufficient to trigger RRP but not SRP exocytosis...
February 13, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28192663/surfactant-free-solid-dispersions-of-hydrophobic-drugs-in-an-amorphous-sugar-matrix-dried-from-an-organic-solvent
#9
Koji Takeda, Yuto Gotoda, Daichi Hirota, Fumihiro Hidaka, Tomo Sato, Tsutashi Matsuura, Hiroyuki Imanaka, Naoyuki Ishida, Koreyoshi Imamura
The technique for homogeneously dispersing hydrophobic drugs in a water-soluble solid matrix (solid dispersion) is a subject that has been extensively investigated in the pharmaceutical industry. Herein, a novel technique for dispersing a solid, without the need to use a surfactant, is reported. A freeze-dried amorphous sugar sample was dissolved in an organic solvent, that contained a soluble model hydrophobic component. The suspension of the sugar and the model hydrophobic component was vacuum foam dried to give a solid powder...
February 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28192423/elucidation-of-molecular-kinetic-schemes-from-macroscopic-traces-using-system-identification
#10
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/28185965/cav1-2-but-not-cav1-3-l-type-calcium-channel-subtype-mediates-nicotine-induced-conditioned-place-preference-in-miceo
#11
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/28140590/effect-of-low-concentration-polymers-on-crystal-growth-in-molecular-glasses-a-controlling-role-for-polymer-segmental-mobility-relative-to-host-dynamics
#12
Chengbin Huang, C Travis Powell, Ye Sun, Ting Cai, Lian Yu
Low-concentration polymers can strongly influence crystal growth in small-molecule glasses, a phenomenon important for improving physical stability against crystallization. We measured the velocity of crystal growth in two molecular glasses, nifedipine (NIF) and o-terphenyl (OTP), each doped with four or five different polymers. For each polymer, the concentration was fixed at 1 wt % and a wide range of molecular weights was tested. We find that a polymer additive can strongly alter the rate of crystal growth, from a 10-fold reduction to a 10-fold increase...
February 15, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28135716/overexpression-of-cardiac-specific-kinase-tnni3k-promotes-mouse-embryonic-stem-cells-differentiation-into-cardiomyocytes
#13
Yin Wang, Shi-Qiang Wang, Li-Peng Wang, Yu-Hong Yao, Chun-Yan Ma, Jin-Feng Ding, Jue Ye, Xian-Min Meng, Rui-Xia Xu, Jian-Jun Li
: Backgroud/Aims: The biological function of cardiac troponin I-interacting kinase (TNNI3K), a cardiac-specific functional kinase, is largely unknown. We investigated the effect of human TNNI3K (hTNNI3K) on the differentiation of mouse embryonic stem cells (mESCs) into cardiomyocytes. METHODS: First, the time-space expression of endogenous Tnni3k was detected by real-time polymerase chain reaction (PCR) and western blotting at 16 different time-points over a period of 28 days...
January 26, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28126850/structural-insights-into-the-atomistic-mechanisms-of-action-of-small-molecule-inhibitors-targeting-the-kca3-1-channel-pore
#14
Hai M Nguyen, Vikrant Singh, Brandon Pressly, David Paul Jenkins, Heike Wulff, Vladimir Yarov-Yarovoy
The calcium-activated potassium channel KCa3.1 constitutes an attractive pharmacological target for immunosuppression, fibroproliferative disorders, atherosclerosis and stroke. However, there currently is no available crystal structure of this medically relevant channel that could be used for structure-assisted drug design. Using the Rosetta molecular modeling suite we generated a molecular model of the KCa3.1 pore and tested the model by first confirming previously mapped binding sites and visualizing the mechanism of TRAM-34, senicapoc and NS6180 inhibition at the atomistic level...
January 26, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28110808/suppression-of-graft-spasm-by-the-particulate-guanylyl-cyclase-activator-in-coronary-bypass-surgery
#15
Takeshi Kinoshita, Masashi Tawa, Tomoaki Suzuki, Yoshinari Aimi, Tohru Asai, Tomio Okamura
BACKGROUND: Spasm of arterial grafts is still a clinical problem in coronary artery bypass surgery. The present study was designed to examine the effect of particulate guanylyl cyclase activator (carperitide) as an antispastic agent in internal thoracic artery and gastroepiploic artery grafts. METHODS: Isolated arterial grafts taken during surgery were studied in organ bath in three ways: the relaxing effect of carperitide on vasoconstrictor-induced precontraction; the inhibitory effect of pretreatment with carperitide on subsequent vasoconstrictor-induced contraction; and the effect of carperitide and nitroglycerin on increase of intracellular cyclic guanosine monophosphate levels...
January 19, 2017: Annals of Thoracic Surgery
https://www.readbyqxmd.com/read/28107550/enhanced-trpc-channel-mediated-ca-2-influx-in-the-cells-with-phospholipase-c-%C3%AE-1-overexpression-its-possible-role-in-coronary-artery-spasm
#16
Kazuo Murakami, Tomohiro Osanai, Makoto Tanaka, Kimitaka Nishizaki, Takahiko Kinjo, Tomohiro Tanno, Yuji Ishida, Akiko Suzuki, Tomohide Endo, Hirofumi Tomita, Ken Okumura
We reported that coronary spasm was induced in the transgenic mice with the increased phospholipase C (PLC)-δ1 activity. We investigated the effect of enhanced PLC-δ1 on Ca(2+) influx and its underlying mechanisms. We used human embryonic kidney (HEK)-293 and coronary arteries-smooth-muscle cells (CASMC). Intracellular free Ca(2+) concentration ([Ca(2+) ]i ) (nM) was measured by fura-2, and Ca(2+) influx was evaluated by the increase in [Ca(2+) ]i after addition of extracellular Ca(2+) . Acetylcholine (ACh) was used to induce Ca(2+) influx...
January 20, 2017: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/28101450/hyponatremic-hypertensive-syndrome-a-retrospective-cohort-study
#17
Devdeep Mukherjee, Rajiv Sinha, Md Shakil Akhtar, Agni Sekhar Saha
AIM: To ascertain the frequency of hyponatremic hypertensive syndrome (HHS) in a cohort of children with hypertensive emergency in a tertiary pediatric hospital. METHODS: A retrospective review was undertaken among children with hypertensive emergency admitted in our tertiary children hospital between June 2014 and December 2015 with an aim to identify any children with HHS. Three children with HHS were identified during this period. RESULTS: The 3 patients with HHS presented with hypertensive emergency...
January 6, 2017: World Journal of Nephrology
https://www.readbyqxmd.com/read/28090225/efficacy-and-safety-of-combination-therapy-consisting-of-angiotensin-ii-type-1-receptor-blocker-calcium-channel-blocker-and-hydrochlorothiazide-in-patients-with-hypertension
#18
Yuhei Shiga, Shin-Ichiro Miura, Kota Motozato, Yuka Yoshimine, Kenji Norimatsu, Tadaaki Arimura, Rie Koyoshi, Joji Morii, Takashi Kuwano, Ken Inoue, Tetsuro Shirotani, Kazuaki Fujisawa, Eiyu Matsunaga, Keijiro Saku
BACKGROUND: Many patients continue to have high blood pressure (BP) even after treatment with high-dose (H)-angiotensin II type 1 receptor blocker (ARB)/calcium channel blocker (CCB) or middle-dose (M)-ARB/CCB/hydrochlorothiazide (HCTZ). METHODS: Thirty-two hypertensive patients who had the use of H-ARB/CCB or M-ARB/CCB/HCTZ were enrolled in this study. We applied a changeover with a switch to H-ARB (telmisartan 80 mg/day)/CCB (amlodipine 5 mg/day or nifedipine CR 40 mg/day)/HCTZ (12...
February 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/28073119/in-vitro-inhibition-of-human-cyp450s-1a2-2c9-3a4-5-2d6-and-2e1-by-grandisin
#19
Maísa Daniela Habenschus, Fernanda de Lima Moreira, Norberto Peporine Lopes, Anderson R M de Oliveira
Grandisin, a lignan isolated from many species of plants, such as Virola surinamensis, is a potential drug candidate due to its biological properties, highlighted by its antitumor and trypanocidal activities. In this study, the inhibitory effects of grandisin on the activities of human cytochrome P450 enzymes were investigated by using human liver microsomes. Results showed that grandisin is a competitive inhibitor of CYP2C9 and a competitive and mechanism-based inhibitor of CYP3A4/5. The apparent Ki value for CYP2C9 was 50...
January 10, 2017: Planta Medica
https://www.readbyqxmd.com/read/28069789/hypotension-induced-by-the-concomitant-use-of-a-calcium-channel-blocker-and-clarithromycin
#20
Sayako Takeuchi, Yuki Kotani, Toshihide Tsujimoto
In the elderly, calcium-channel blockers are the first-line treatment for hypertension, and macrolides are commonly prescribed antibiotics. Here we report a 78-year-old man taking nifedipine, diltiazem and carvedilol who presented with persistent hypotension and bradycardia after clarithromycin was prescribed. He was diagnosed with drug-induced hypotension and treated with fluid resuscitation and vasoactive agents. His symptoms gradually improved. He was transferred out of the intensive care unit 3 days after hospitalisation...
January 9, 2017: BMJ Case Reports
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