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Daniel Leon-Aparicio et al.
Cell calcium, 65, 91-101 (2017-02-10)
We have studied in HeLa cells the molecular nature of the 2-APB induced ER Ca
Lin Lin et al.
Otolaryngology--head and neck surgery : official journal of American Academy of Otolaryngology-Head and Neck Surgery, 153(3), 461-467 (2015-06-19)
Glucocorticoids are considered the main treatment option for chronic rhinosinusitis with nasal polyps (CRSwNP), but their effect rate ranges from 60.9% to 80%. Novel therapeutic means should be studied. The purpose of this study was to investigate the expression of...
Mine Islimye Taskin et al.
European journal of obstetrics, gynecology, and reproductive biology, 178, 74-79 (2014-05-06)
The aim of this study is to evaluate the effects of 2-aminoethoxydiphenyl borate (2-APB) as an antioxidant and analyze biochemical and histopathologic changes in experimental ischemia-reperfusion (I/R) injury in rat ovaries. Thirty female rats were utilized to create four groups....
M Karademir et al.
Bratislavske lekarske listy, 119(12), 752-756 (2019-01-29)
The objective of this study was to determine the neuroprotective effects of 2-aminoethyl diphenyl-borinate (2-APB) on the brains of rats with experimentally-induced severe acute pancreatitis. Thirty Spraque-Dawley male rats with an average weight of 200-250 grams were randomly divided into...
Kenji Takahashi et al.
Experimental cell research, 323(2), 337-345 (2014-03-19)
2-Aminoethoxydiphenyl borate (2-APB) is used as a pharmacological tool because it antagonizes inositol 1,4,5-trisphosphate receptors and store-operated Ca(2+) (SOC) channels, and activates some TRP channels. Recently, we reported that 2-APB enhanced the increase in cytotoxic [Ca(2+)]i, resulting in cell death...
Achille Schild et al.
International journal of molecular sciences, 21(16) (2020-08-09)
Calcium ions regulate a wide array of physiological functions including cell differentiation, proliferation, muscle contraction, neurotransmission, and fertilization. The endoplasmic reticulum (ER) is the major intracellular Ca2+ store and cellular events that induce ER store depletion (e.g., activation of inositol...
Michal Bencze et al.
European journal of pharmacology, 765, 533-540 (2015-09-20)
Transient receptor potential (TRP) channels are proposed to contribute to membrane depolarization and Ca2+ influx into vascular smooth muscle (VSM) cells. Our aim was to study the effects of widely used broad-range TRP channel inhibitors--2-aminoethoxydiphenyl borate (2-APB), flufenamic acid (FFA)...
Xiao-Xuan Yu et al.
Acta pharmacologica Sinica, 42(2), 290-300 (2020-08-05)
Cutaneous T-cell lymphoma (CTCL) is characterized by a heterogeneous group of extranodal non-Hodgkin lymphomas, in which monoclonal T lymphocytes infiltrate the skin. LW-213, a derivative of wogonin, was found to induce cell apoptosis in chronic myeloid leukemia (CML). In this...
Marlena Zyśk et al.
Antioxidants (Basel, Switzerland), 9(6) (2020-06-18)
N-acetylaspartate is produced by neuronal aspartate N-acetyltransferase (NAT8L) from acetyl-CoA and aspartate. In cholinergic neurons, acetyl-CoA is also utilized in the mitochondrial tricarboxylic acid cycle and in acetylcholine production pathways. While aspartate has to be shared with the malate-aspartate shuttle...
Alaeddine Djillani et al.
Biochimica et biophysica acta, 1843(10), 2341-2347 (2014-03-25)
2-Aminoethyl diphenylborinate (2-APB) is a well-known effector of the store-operated Ca(2+) entry of several cell types such as immune cells, platelets and smooth muscle cells. 2-APB has a dual effect: potentiation at 1-5μM and inhibition at >30μM. Unfortunately, it is...
Eunan Hendron et al.
Cell calcium, 56(6), 482-492 (2014-12-03)
The coupling of ER Ca(2+)-sensing STIM proteins and PM Orai Ca(2+) entry channels generates "store-operated" Ca(2+) signals crucial in controlling responses in many cell types. The dimeric derivative of 2-aminoethoxydiphenyl borinate (2-APB), DPB162-AE, blocks functional coupling between STIM1 and Orai1...
Leopoldo Beltrán et al.
Frontiers in pharmacology, 4, 63-63 (2013-05-31)
Two-pore domain K(+) (KCNK, K2P) channels underlie the "leak" (background) potassium conductance in many types of excitable cells. They oppose membrane depolarization and cell excitability. These channels have been reported to be modulated by several physical and chemical stimuli. The...
Kazuhiro Kurokawa et al.
Journal of neurochemistry, 131(6), 836-847 (2014-09-16)
This study involved mice that received 4 days of ethanol (EtOH) vapor inhalation and then were assessed for type 1 inositol 1,4,5-trisphosphate receptor (IP3 Rs-1) expression and the development of EtOH-induced place preference at various time points in withdrawal. IP3...
Huma Saleem et al.
British journal of pharmacology, 171(13), 3298-3312 (2014-03-19)
Inositol 1,4,5-trisphosphate receptors (IP3 Rs) are intracellular Ca(2+) channels. Interactions of the commonly used antagonists of IP3Rs with IP3R subtypes are poorly understood. IP3-evoked Ca(2+) release from permeabilized DT40 cells stably expressing single subtypes of mammalian IP3R was measured using...
Jorge Navarro-Dorado et al.
Biochemical and biophysical research communications, 445(1), 84-88 (2014-02-11)
Phenylephrine (PE)-induced oscillatory fluctuations in intracellular Ca(2+) concentration ([Ca(2+)]i) of vascular smooth muscle have been observed in many blood vessels isolated from a wide variety of mammals. Paradoxically, until recently similar observations in humans have proven elusive. In this study...
Shin-ichiro Hirai et al.
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics, 31(9), 570-584 (2015-08-28)
To investigate the efficacy of 2-phenyl-APB-144 (APB)-induced retinopathy in a rat model and its underlying mechanisms, with a particular focus on retinal pigment epithelium (RPE) degeneration. Electroretinograms (ERGs) were evaluated in APB-administered rats. In ARPE-19 cells, cathepsin, and autophagy marker...
Gui-Lan Chen et al.
British journal of pharmacology, 167(6), 1232-1243 (2012-06-01)
Fenamate analogues, econazole and 2-aminoethoxydiphenyl borate (2-APB) are inhibitors of transient receptor potential melastatin 2 (TRPM2) channels and are used as research tools. However, these compounds have different chemical structures and therapeutic applications. Here we have investigated the pharmacological profile...
Linda Lefièvre et al.
The Biochemical journal, 448(2), 189-200 (2012-09-05)
Ca2+i signalling is pivotal to sperm function. Progesterone, the best-characterized agonist of human sperm Ca2+i signalling, stimulates a biphasic [Ca2+]i rise, comprising a transient and subsequent sustained phase. In accordance with recent reports that progesterone directly activates CatSper, the [Ca2+]i...
Hao Wei et al.
Cell death discovery, 6, 10-10 (2020-03-07)
Activated, procoagulant platelets shed phosphatidylserine (PS)-exposing extracellular vesicles (EVs) from their surface in a Ca2+- and calpain-dependent manner. These PS-exposing EVs are prothrombotic and proinflammatory and are found at elevated levels in many cardiovascular and metabolic diseases. How PS-exposing EVs...
Hongzhen Hu et al.
Proceedings of the National Academy of Sciences of the United States of America, 106(5), 1626-1631 (2009-01-24)
Temperature-activated transient receptor potential ion channels (thermoTRPs) are polymodal detectors of various stimuli including temperature, voltage, and chemicals. To date, it is not known how TRP channels integrate the action of such disparate stimuli. Identifying specific residues required for channel-activation...
M G Rae et al.
Neurochemistry international, 60(6), 543-554 (2012-03-01)
Although transient receptor potential (TRP) channel biology research has expanded rapidly in recent years, the field is hampered by the widely held, but relatively poorly investigated, belief that most of the pharmacological tools used to investigate TRP channel function may...
Jun-Ichi Goto et al.
Cell calcium, 47(1), 1-10 (2009-12-01)
Store-operated calcium entry (SOCE) or calcium release-activated calcium current (I(CRAC)) is a critical pathway to replenish intracellular calcium stores, and plays indispensable roles in cellular functions such as antigen-induced T lymphocyte activation. Despite the importance of I(CRAC) in cellular functions...
Iain M McIntyre et al.
Journal of analytical toxicology, 39(2), 156-159 (2014-11-29)
A 20-year-old man, a college student, became unresponsive in front of his girlfriend. He was known to consume alcohol and take an unknown drug at some point while in attendance at a local music festival earlier in the day/evening. Upon...
Rachel E Jarrard et al.
Molecular pharmacology, 83(1), 191-205 (2012-10-17)
Tolbutamide and gliclazide block the K(ATP) channel K(ir)6.2/Sur1, causing membrane depolarization and stimulating insulin secretion in pancreatic beta cells. We examined the ability of the EPAC-selective cAMP analog 8-pCPT-2'-O-Me-cAMP-AM to potentiate the action of these drugs and the mechanism that...
Kuo Du et al.
Toxicology and applied pharmacology, 273(3), 484-491 (2013-09-28)
Acetaminophen (APAP) hepatotoxicity is the leading cause of acute liver failure in the US. Although many aspects of the mechanism are known, recent publications suggest that gap junctions composed of connexin32 function as critical intercellular communication channels which transfer cytotoxic...
Gerald Thiel et al.
Biochemical pharmacology, 170, 113678-113678 (2019-10-28)
Transient receptor potential melastatin-8 (TRPM8) channels are activated by cold temperature, menthol and icilin, leading to cold sensation. TRPM8 activation is connected with various diseases, indicating that a specific pharmacological antagonist, allowing nongenetic channel suppression, would be a valuable tool...
Felix Hohendanner et al.
Channels (Austin, Tex.), 9(3), 129-138 (2015-04-22)
In rabbit atrial myocytes Ca signaling has unique features due to the lack of transverse (t) tubules, the spatial arrangement of mitochondria and the contribution of inositol-1,4,5-trisphosphate (IP3) receptor-induced Ca release (IICR). During excitation-contraction coupling action potential-induced elevation of cytosolic...
Hirofumi Morihara et al.
PloS one, 12(12), e0189948-e0189948 (2017-12-22)
Excessive levels of reactive oxygen species (ROS) and impaired Ca2+ homeostasis play central roles in the development of multiple cardiac pathologies, including cell death during ischemia-reperfusion (I/R) injury. In several organs, treatment with 2-aminoethoxydiphenyl borate (2-APB) was shown to have...
Rainer Schindl et al.
The Journal of biological chemistry, 283(29), 20261-20267 (2008-05-24)
Stim1 in the endoplasmic reticulum and the three Orai (also termed CRACM) channels in the plasma-membrane are main components of native Ca(2+) release-activated Ca(2+) channels. A pharmacological hallmark of these channels is their distinct sensitivity to 2-aminoethoxydiphenyl borate (2-APB). Here...
Qihai Gu et al.
American journal of physiology. Lung cellular and molecular physiology, 288(5), L932-L941 (2005-01-18)
This study was carried out to determine the effect of 2-aminoethoxydiphenyl borate (2-APB), a common activator of transient receptor potential vanilloid (TRPV) type 1, 2, and 3 channels, on cardiorespiratory reflexes, pulmonary C fiber afferents, and isolated pulmonary capsaicin-sensitive neurons....
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