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https://www.readbyqxmd.com/read/29684576/zd7288-and-mibefradil-inhibit-the-myogenic-heartbeat-in-daphnia-magna-indicating-its-dependency-on-hcn-and-t-type-calcium-ion-channels
#1
Thomas J Pirtle, Troy L Carr, Tanisha Khurana, Grace Meeker
Daphnia magna heartbeat is myogenic-originating within the animal's heart. However, the mechanism for this myogenic automaticity is unknown. The mechanism underlying the automaticity of vertebrate myogenic hearts involves cells (pacemaker cells), which have a distinct set of ion channels that include hyperpolarization activated cyclic nucleotide-gated (HCN) and T-type calcium ion channels. We hypothesized that these ion channels also underlie the automatic myogenic heartbeat of Daphnia magna. The drugs, ZD7288 and mibefradil dihydrochloride, block HCN and T-type calcium ion channels respectively...
April 20, 2018: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/29556214/calcium-channels-in-postnatal-development-of-rat-pancreatic-beta-cells-and-their-role-in-insulin-secretion
#2
Neivys García-Delgado, Myrian Velasco, Carmen Sánchez-Soto, Carlos Manlio Díaz-García, Marcia Hiriart
Pancreatic beta cells during the first month of development acquire functional maturity, allowing them to respond to variations in extracellular glucose concentration by secreting insulin. Changes in ionic channel activity are important for this maturation. Within the voltage-gated calcium channels (VGCC), the most studied channels are high-voltage-activated (HVA), principally L-type; while low-voltage-activated (LVA) channels have been poorly studied in native beta cells. We analyzed the changes in the expression and activity of VGCC during the postnatal development in rat beta cells...
2018: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29472842/accumulation-of-ca-v-3-2-t-type-calcium-channels-in-the-uninjured-sural-nerve-contributes-to-neuropathic-pain-in-rats-with-spared-nerve-injury
#3
Wen Chen, Ye-Nan Chi, Xue-Jing Kang, Qing-Ying Liu, Hao-Lin Zhang, Zhi-Hua Li, Zi-Fang Zhao, Yin Yang, Li Su, Jie Cai, Fei-Fei Liao, Ming Yi, You Wan, Feng-Yu Liu
Injuries to peripheral nerve fibers induce neuropathic pain. But the involvement of adjacent uninjured fibers to pain is not fully understood. The present study aims to investigate the possible contribution of Cav 3.2 T-type calcium channels in uninjured afferent nerve fibers to neuropathic pain in rats with spared nerve injury (SNI). Aβ-, Aδ- and C-fibers of the uninjured sural nerve were sensitized revealed by in vivo single-unit recording, which were accompanied by accumulation of Cav 3.2 T-type calcium channel proteins shown by Western blotting...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29343521/t-type-ca2-channels-t-for-targetable
#4
REVIEW
Marta C Sallán, Anna Visa, Soni Shaikh, Mireia Nàger, Judit Herreros, Carles Cantí
In the past decade, T-type Ca2+ channels (TTCC) have been unveiled as key regulators of cancer cell biology and thus have been proposed as chemotherapeutic targets. Indeed, in vitro and in vivo studies indicate that TTCC pharmacologic blockers have a negative impact on the viability of cancer cells and reduce tumor size, respectively. Consequently mibefradil, a TTCC blocker approved in 1997 as an antihypertensive agent but withdrawn in 1998 because of drug-drug interactions, was granted 10 years later the orphan drug status by the FDA to investigate its efficacy against brain, ovary, and pancreatic cancer...
January 17, 2018: Cancer Research
https://www.readbyqxmd.com/read/29207174/calcium-channels-are-involved-in-ephb-ephrinb-reverse-signaling%C3%A2-induced-apoptosis-in-a-rat-chronic-ocular-hypertension-model
#5
Lingdan Dong, Xianglin Cheng, Long Zhou, Yanhong Hu
Erythropoietin-producing hepatocyte receptor B (EphB)/ephrinB reverse signaling has been revealed to be activated in chronic ocular hypertension (COH) by increasing the apoptosis of retinal ganglion cells (RGCs). However, the exact mechanism is not well understood. The present study investigated the involvement of Ca2+ channels in the apoptosis of RGCs induced by EphB/ephrinB reverse signaling in a rat CHO model, which was established by cauterizing 3 out of the 4 episcleral veins. The expression levels of four voltage‑gated Ca2+ channel subunits (Cav3...
February 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29183797/increase-in-ca-2-current-by-sustained-camp-levels-enhances-proliferation-rate-in-gh3-cells
#6
Andréia Laura Rodrigues, Marcella Brescia, Andreas Koschinski, Thaís Helena Moreira, Ryan T Cameron, George Baillie, Paulo S L Beirão, Manuela Zaccolo, Jader S Cruz
AIMS: Ca2+ and cAMP are important intracellular modulators. In order to generate intracellular signals with various amplitudes, as well as different temporal and spatial properties, a tightly and precise control of these modulators in intracellular compartments is necessary. The aim of this study was to evaluate the effects of elevated and sustained cAMP levels on voltage-dependent Ca2+ currents and proliferation in pituitary tumor GH3 cells. MAIN METHODS: Effect of long-term exposure to forskolin and dibutyryl-cyclic AMP (dbcAMP) on Ca2+ current density and cell proliferation rate were determined by using the whole-cell patch-clamp technique and real time cell monitoring system...
January 1, 2018: Life Sciences
https://www.readbyqxmd.com/read/29167643/post-inflammatory-ileitis-induces-non-neuronal-purinergic-signaling-adjustments-of-cholinergic-neurotransmission-in-the-myenteric-plexus
#7
Cátia Vieira, Fátima Ferreirinha, Maria T Magalhães-Cardoso, Isabel Silva, Patrícia Marques, Paulo Correia-de-Sá
Uncoupling between ATP overflow and extracellular adenosine formation changes purinergic signaling in post-inflammatory ileitis. Adenosine neuromodulation deficits were ascribed to feed-forward inhibition of ecto-5'-nucleotidase/CD73 by high extracellular adenine nucleotides in the inflamed ileum. Here, we hypothesized that inflammation-induced changes in cellular density may also account to unbalance the release of purines and their influence on [3 H]acetylcholine release from longitudinal muscle-myenteric plexus preparations of the ileum of 2,4,6-trinitrobenzenesulfonic acid (TNBS)-treated rats...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29135027/acrosomal-alkalization-triggers-ca-2-release-and-acrosome-reaction-in-mammalian-spermatozoa
#8
Julio C Chávez, José L De la Vega-Beltrán, Omar José, Paulina Torres, Takuya Nishigaki, Claudia L Treviño, Alberto Darszon
The sperm acrosome reaction (AR), an essential event for mammalian fertilization, involves Ca2+ permeability changes leading to exocytosis of the acrosomal vesicle. The acrosome, an intracellular Ca2+ store whose luminal pH is acidic, contains hydrolytic enzymes. It is known that acrosomal pH (pHacr ) increases during capacitation and this correlates with spontaneous AR. Some AR inducers increase intracellular Ca2+ concentration ([Ca2+ ]i ) through Ca2+ release from internal stores, mainly the acrosome. Catsper, a sperm specific Ca2+ channel, has been suggested to participate in the AR...
June 2018: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29044427/genomic-identification-expression-profiling-and-functional-characterization-of-catsper-channels-in-the-bovine
#9
Gillian P Johnson, Anne-Marie English, Sinead Cronin, David A Hoey, Kieran G Meade, Sean Fair
Cation channels of sperm (CatSper) are sperm-specific calcium channels with identified roles in the regulation of sperm function in humans, mice, and horses. We sought to employ a comparative genomics approach to identify conserved CATSPER genes in the bovine genome, and profile their expression in reproductive tissue. We hypothesized that CATSPER proteins expressed in bull testicular tissue mediates sperm hyperactivation and their rheotactic response in the reproductive tract of the cow. Bioinformatic analysis identified all four known CATSPER genes (CATSPER 1-4) in the bovine genome, and profiling by quantitative real-time polymerase chain reaction identified site-specific variation in messenger ribonucleic acid (mRNA) expression for all four genes along the reproductive tract of the bull...
August 1, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/28934223/ursodeoxycholic-acid-prevents-ventricular-conduction-slowing-and-arrhythmia-by-restoring-t-type-calcium-current-in-fetuses-during-cholestasis
#10
Oladipupo Adeyemi, Anita Alvarez-Laviada, Francisca Schultz, Effendi Ibrahim, Michael Trauner, Catherine Williamson, Alexey V Glukhov, Julia Gorelik
BACKGROUND: Increased maternal serum bile acid concentrations in intrahepatic cholestasis of pregnancy (ICP) are associated with fetal cardiac arrhythmias. Ursodeoxycholic acid (UDCA) has been shown to demonstrate anti-arrhythmic properties via preventing ICP-associated cardiac conduction slowing and development of reentrant arrhythmias, although the cellular mechanism is still being elucidated. METHODS: High-resolution fluorescent optical mapping of electrical activity and electrocardiogram measurements were used to characterize effects of UDCA on one-day-old neonatal and adult female Langendorff-perfused rat hearts...
2017: PloS One
https://www.readbyqxmd.com/read/28877214/direct-versus-indirect-actions-of-ghrelin-on-hypothalamic-npy-neurons
#11
Hiroshi Hashiguchi, Zhenyu Sheng, Vanessa Routh, Volodymyr Gerzanich, J Marc Simard, Joseph Bryan
OBJECTIVES: Assess direct versus indirect action(s) of ghrelin on hypothalamic NPY neurons. MATERIALS AND METHODS: Electrophysiology was used to measure ion channel activity in NPY-GFP neurons in slice preparations. Ca2+ imaging was used to monitor ghrelin activation of isolated NPY GFP-labeled neurons. Immunohistochemistry was used to localize Trpm4, SUR1 and Kir6.2 in the hypothalamus. RESULTS: Acylated ghrelin depolarized the membrane potential (MP) of NPY-GFP neurons in brain slices...
2017: PloS One
https://www.readbyqxmd.com/read/28713955/altered-axon-initial-segment-in-hippocampal-newborn-neurons-associated-with-recurrence-of-temporal-lobe-epilepsy-in-rats
#12
Tian-Tian Liu, Li Feng, Heng-Fang Liu, Yi Shu, Bo Xiao
Hippocampal neurogenesis in temporal lobe epilepsy (TLE) may result in alteration of the excitability of neurons, which contributes to spontaneous recurrent seizures. Axon initial segment (AIS) structural and functional plasticity is important in the control of neuronal excitability. It remains to be elucidated whether the plasticity of AIS occurs in hippocampal newly‑generated neurons that are involved in recurrent seizures following pilocarpine‑induced status epilepticus (SE). The present study first established a pilocarpine‑induced TLE rat model to assess the features of newborn neurons and AIS plasticity alterations using double immunofluorescence staining of Ankyrin G and doublecortin (DCX)...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28650687/mibefradil-inhibition-of-the-cole-moore-shift-and-k-conductance-of-the-tumor-related-kv10-1-channel
#13
F Gómez-Lagunas, C Barriga-Montoya
No abstract text is available yet for this article.
September 3, 2017: Channels
https://www.readbyqxmd.com/read/28603637/t-type-voltage-gated-ca-2-channels-do-not-contribute-to-the-negative-feedback-regulation-of-myogenic-tone-in-murine-superior-epigastric-arteries
#14
Brendan Mullan, Jessica Pettis, William F Jackson
T-type voltage-gated Ca(2+) channels (CaV3.2 VGCC) have been hypothesized to control spontaneous transient outward currents (STOCs) through large-conductance Ca(2+)-activated K(+) channels (BKCa), and contribute to the negative-feedback regulation of myogenic tone. We tested this hypothesis in superior epigastric arteries (SEAs) isolated from male C57BL/6 mice. SEAs were isolated and enzymatically dissociated to obtain single smooth muscle cells (SMCs) for whole-cell recording of paxilline-sensitive (PAX, 1 μmol/L) STOCs at -30 mV, or cannulated and studied by pressure myography (80 cm H2O, 37°C)...
June 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28533239/plasmodium-falciparum-and-plasmodium-vivax-demonstrate-contrasting-chloroquine-resistance-reversal-phenotypes
#15
Grennady Wirjanata, Irene Handayuni, Pak Prayoga, Leo Leonardo, Dwi Apriyanti, Leily Trianty, Ruland Wandosa, Basbak Gobay, Enny Kenangalem, Jeanne Rini Poespoprodjo, Rintis Noviyanti, Dennis E Kyle, Qin Cheng, Ric N Price, Jutta Marfurt
High-grade chloroquine (CQ) resistance has emerged in both Plasmodium falciparum and P. vivax The aim of the present study was to investigate the phenotypic differences of CQ resistance in both of these species and the ability of known CQ resistance reversal agents (CQRRAs) to alter CQ susceptibility. Between April 2015 and April 2016, the potential of verapamil (VP), mibefradil (MF), L703,606 (L7), and primaquine (PQ) to reverse CQ resistance was assessed in 46 P. falciparum and 34 P. vivax clinical isolates in Papua, Indonesia, where CQ resistance is present in both species, using a modified schizont maturation assay...
August 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28512247/targetable-t-type-calcium-channels-drive-glioblastoma
#16
Ying Zhang, Nichola Cruickshanks, Fang Yuan, Baomin Wang, Mary Pahuski, Julia Wulfkuhle, Isela Gallagher, Alexander F Koeppel, Sarah Hatef, Christopher Papanicolas, Jeongwu Lee, Eli E Bar, David Schiff, Stephen D Turner, Emanuel F Petricoin, Lloyd S Gray, Roger Abounader
Glioblastoma (GBM) stem-like cells (GSC) promote tumor initiation, progression, and therapeutic resistance. Here, we show how GSCs can be targeted by the FDA-approved drug mibefradil, which inhibits the T-type calcium channel Cav3.2. This calcium channel was highly expressed in human GBM specimens and enriched in GSCs. Analyses of the The Cancer Genome Atlas and REMBRANDT databases confirmed upregulation of Cav3.2 in a subset of tumors and showed that overexpression associated with worse prognosis. Mibefradil treatment or RNAi-mediated attenuation of Cav3...
July 1, 2017: Cancer Research
https://www.readbyqxmd.com/read/28438566/t-type-voltage-gated-calcium-channels-are-involved-in-endothelium-dependent-relaxation-of-mice-pulmonary-artery
#17
Guillaume Gilbert, Arnaud Courtois, Mathilde Dubois, Laure-Anne Cussac, Thomas Ducret, Philippe Lory, Roger Marthan, Jean-Pierre Savineau, Jean-François Quignard
In pulmonary arterial endothelial cells, Ca(2+) channels and intracellular Ca(2+) concentration ([Ca(2+)]i) control the release of vasorelaxant factors such as nitric oxide and are involved in the regulation of pulmonary arterial blood pressure. The present study was undertaken to investigate the implication of T-type voltage-gated Ca(2+) channels (T-VGCCs, Cav3.1 channel) in the endothelium-dependent relaxation of intrapulmonary arteries. Relaxation was quantified by means of a myograph in wild type and Cav3...
August 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28429070/properties-of-synchronous-spontaneous-ca-2-transients-in-the-mural-cells-of-rat-rectal-arterioles
#18
Retsu Mitsui, Hikaru Hashitani
Synchrony of spontaneous Ca(2+) transients among venular mural cells (smooth muscle cells and pericytes) in visceral organs relies on the intercellular spread of L-type voltage-dependent Ca(2+) channel (LVDCC)-dependent depolarisations. However, the mechanisms underlying the synchrony of spontaneous Ca(2+) transients between arteriolar mural cells are less understood. The spontaneous intracellular Ca(2+) dynamics of arteriolar mural cells in the rat rectal submucosa were visualised by Cal-520 Ca(2+) imaging to analyse their synchrony...
April 21, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28371832/timed-sequential-therapy-of-the-selective-t-type-calcium-channel-blocker-mibefradil-and-temozolomide-in-patients-with-recurrent-high-grade-gliomas
#19
Matthias Holdhoff, Xiaobu Ye, Jeffrey G Supko, Louis B Nabors, Arati S Desai, Tobias Walbert, Glenn J Lesser, William L Read, Frank S Lieberman, Martin A Lodge, Jeffrey Leal, Joy D Fisher, Serena Desideri, Stuart A Grossman, Richard L Wahl, David Schiff
Background: Mibefradil (MIB), previously approved for treatment of hypertension, is a selective T-type calcium channel blocker with preclinical activity in high-grade gliomas (HGGs). To exploit its presumed mechanism of impacting cell cycle activity (G1 arrest), we designed a phase I study to determine safety and the maximum tolerated dose (MTD) of MIB when given sequentially with temozolomide (TMZ) in recurrent (r)HGG. Methods: Adult patients with rHGG ≥3 months from TMZ for initial therapy received MIB in 4 daily doses (q...
June 1, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/28364016/reduced-membrane-cholesterol-limits-pulmonary-endothelial-ca-2-entry-after-chronic-hypoxia
#20
Bojun Zhang, Jay S Naik, Nikki L Jernigan, Benjimen R Walker, Thomas C Resta
Chronic hypoxia (CH)-induced pulmonary hypertension is associated with diminished production of endothelium-derived Ca(2+)-dependent vasodilators such as nitric oxide. Interestingly, ATP-induced endothelial Ca(2+) entry as well as membrane cholesterol (Chol) are decreased in pulmonary arteries from CH rats (4 wk, barometric pressure = 380 Torr) compared with normoxic controls. Store-operated Ca(2+) entry (SOCE) and depolarization-induced Ca(2+) entry are major components of the response to ATP and are similarly decreased after CH...
June 1, 2017: American Journal of Physiology. Heart and Circulatory Physiology
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