*  T-TYPE CALCIUM CHANNEL BLOCKER - Patent application
1. A method for preventing or treating hypercardia, heart failure, cardiomyopathy, atrial fibrillation, tachyarrhythmia, arterial sclerosis, nephritis, nephropathy, renal disorder, renal insufficiency, inflammation, edema, hyper-aldosteronism, neurogenic pain, epilepsy or cancer, comprising:administering to a subject in need thereof an effective amount of a T-type calcium channel blocker having a nitrogen-containing hetero ring moiety of formula (1) ##STR00015## or a pharmaceutically acceptable salt thereof,wherein Ar1 of formula (1) is a substituent selected from the group consisting of a phenyl group, a pyridyl group, a furyl group or a 2,1,3-benzoxadiazol-4-yl group;wherein the Ar1 substituent may be optionally substituted with one or two substituents selected from the group consisting of NO2, CF3, Br, Cl, F, C1-20 alkyl group, OH, OR6, OCHF2, COOR6, NH2, NHR6, NR6R7, CONH2, CONHR6, CONR6R7, COSR6, SR6, S(O)R6, S(O)2R6, SO3H, SO3R6, SO2NH2, SO2NHR6, SO2NR6R7, CN and ...
*  AID 504579 - Inhibitors of T-Type Calcium Channels (rat DRG neuron currents) - PubChem
BioAssay record AID 504579 submitted by Vanderbilt Screening Center for GPCRs, Ion Channels and Transporters: Inhibitors of T-Type Calcium Channels (rat DRG neuron currents).
*  Neurotrophin-4 modulates the mechanotransducer Cav3.2 T-type calcium current in mice down-hair neurons | Biochemical Journal
The T-type Ca2+ channel Cav3.2 is expressed in nociceptive and mechanosensitive sensory neurons. The mechanosensitive D-hair (down-hair) neurons, which innervate hair follicles, are characterized by a large-amplitude Cav3.2 T-current involved in the amplification of slow-moving stimuli. The molecules and signalling pathways that regulate T-current expression in mechanoreceptors are unknown. In the present study, we investigated the effects of NT-4 (neurotrophin-4) on Cav3.2 T-current expression in D-hair neurons in vitro. Interruption of the supply of NT-4 with peripheral nerve axotomy induced a non-transcriptional decrease in the T-current amplitude of fluorogold-labelled axotomized sensory neurons. The T-current amplitude was restored by incubation with NT-4. Deletion of NT-4 through genetic ablation resulted in a similar selective loss of the large-amplitude T-current in NT-4−/− sensory neurons, which was rescued by the addition of NT-4. NT-4 had no effect on the ...
*  Epilepsy drugs could treat Alzheimer's and Parkinson's
They found that neurons showed an increase in viability after treatment with either L-type or T-type calcium channel inhibitors. Furthermore, neurons in the long-term and short-term cultures were protected, respectively, by L-type and T-type calcium channel blockers, suggesting that more than one calcium-signaling mechanism exists to regulate long- and short-term neuron survival.. There are presently no effective medications for age-related neurodegeneration. Bao said "Our data provides implications for the use of this family of anti-epileptic drugs in developing new treatments for neuronal injury, and for the need of further studies of the use of such drugs in age-related neurodegenerative disorders.". 1. Neuroprotective effects of blockers for T-type calcium channels ...
*  Zalicus Successfully Completes Phase 1 Single Ascending Dose Study With Z944 , A Novel, Oral T-Type Calcium Channel Blocker -...
Zalicus Inc. (NASDAQ: ZLCS), a biopharmaceutical company that discovers and develops novel treatments for patients suffering from pain and immuno-inflammatory diseases, today announced that it is has ......ZLCS
*  Abstract 788: Blockade Of T-type Calcium Channels Attenuates Smooth Muscle Cell Migration, Neointimal Formation, And Oxygen...
Ca2+ influx through voltage-dependent Ca2+ channels regulates vascular remodeling and contraction. However, the role of T-type Ca2+ channels (TCCs) has remained unknown in the ductus arteriosus (DA). Here we hypothesized that Ca2+ influx via TCC contributed to DA closure through promoting neointimal cushion formation and oxygen-induced vascular contraction. Quantitative RT-PCR analysis revealed that α1G, a TCC subtype, was significantly up-regulated in rat neonatal DA tissues at birth and in DA smooth muscle cells (SMCs) that were exposed to oxygen. The expression of α1G mRNA was higher in DA than in the aorta. Immunohistlogical analysis revealed that α1G was localized predominantly to the region of intimal thickening in fetal DA at term and to the central core of neonatal DA at birth. To examine the effects of blockade of TCCs, we used α1G-specific siRNA or R(−)-efonidipine, a highly selective TCC blocker that was recently developed. ...
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*  Voltage-dependent T-type calcium channel subunit alpha-1G - DrugBank
This project is supported by the Canadian Institutes of Health Research (award #111062), Alberta Innovates - Health Solutions, and by The Metabolomics Innovation Centre (TMIC), a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by Genome Alberta, Genome British Columbia, and Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $900 million in funding from the federal government. Maintenance, support, and commercial licensing is provided by OMx Personal Health Analytics, Inc. ...
*  A Cav3.2 T-Type Calcium Channel Point Mutation Has Splice-Variant-Specific Effects on Function and Segregates with Seizure...
Correspondence should be addressed to either of the following: Terence O'Brien, Department of Medicine (Royal Melbourne Hospital/Western Hospital), The University of Melbourne, 4th Floor, Clinical Sciences Building, Royal Melbourne Hospital, Royal Parade, Parkville, Victoria 3050, Australia, obrientj{at}unimelb.edu.au; or Terrance Snutch, Michael Smith Laboratories, The University of British Columbia, 301-2185 East Mall, Vancouver, British Columbia, Canada V6T 1Z4, snutch{at}msl.ubc.ca ...
*  T-Type Calcium Channels | Application of Computational Methods for the Design of BACE-1 Inhibitors
There is certainly increasing demand for biomedical implants to improve skeletal defects due to trauma disease or genetic disorder. the original adherence of a lot more cells didn't lead to previously nutrient formation on the cell-implant user interface. From the 84 cell adhesion and matrix-focused pathway genes an up- or down-regulation of a complete of 15 genes such as for example integrin substances integrin alpha M and integrin alpha 7 and 8 was observed recommending a modulating influence on these adhesion substances by the purchased FA surface area weighed against the disordered. Osteocalcin appearance as well as the nutrient nodule development are most noticeable over the FA areas after osteogenic induction (OI) for 7 weeks. The binding from the purchased FA areas to the steel with and without OI was considerably greater than that of the disordered FA areas with OI. Many significantly even with no OI dietary supplement the MG-63 cells harvested on FA ...
*  T-Type Calcium Channels | PI3-kinase inhibitors in lymphoma
G-protein-coupled receptors (GPCRs), which constitute the largest category of cell surface area receptors, were considered to work as monomers originally, but are actually recognized as having the ability to act in an array of oligomeric states and even, it really is known how the oligomerization condition of the GPCR may modulate its function and pharmacology. summarize the most recent developments which have been produced in the methods utilized to review GPCR oligomerization and present TAK-285 a synopsis of their software. [33]. BN-PAGE BN-PAGE, produced by Sch?gger and von Jagow [34] was TAK-285 most likely the first solution to allow electrophoretic parting of intact respiratory proteins complexes through the combined usage of mild detergents and Coomassie Blue dye as opposed to the highly denaturing TAK-285 detergent SDS (Shape 2A). Therefore, a mild solubilization method produces protein complexes within their indigenous areas [35]. Although, Coomassie Blue can be used since it binds to ...
*  Expression of L-type (α1D subunit) and T-type (α1G and α1H subunit) Ca2+ channels in epithelial-derived human breast cancer...
Using the video imaging technique this group has previously reported that regulatory volume decrease (RVD) in ZR-75-1 cells is Ca2+ dependent. RVD was inhibited in the absence of external Ca2+ and in the presence of voltage-gated Ca2+ channel inhibitors, nifedipine (L-type) and flunarizine (T-type; Ashes et al. 2002). These results suggested that external Ca2+ entered the cell via voltage-gated L- and/or T-type Ca2+ channels. In this study, the expression of L- and T-type channels was investigated in ZR-75-1 cells using reverse transcriptase-polymerase chain reaction (RT-PCR). The α1C and α1D are subunits of the L-type Ca2+ channel. The α1C subunit is expressed in cardiac muscle and the α1D subunit in the CNS and endocrine cells, where it may have a role in stimulus-secretion coupling. The α1G, α1H and α1I subunits have been cloned and display biophysical and pharmacological ...
*  CACNA1I (calcium voltage-gated channel subunit alpha1 I) - Rat Genome Database
This gene encodes the pore-forming alpha subunit of a voltage gated calcium channel. The encoded protein is a member of a subfamily of calcium channels referred to as is a low voltage-activated, T-type, calcium channel. The channel encoded by this protein is characterized by a slower activation and inactivation compared to other T-type calcium channels. This protein may be involved in calcium signaling in neurons. Alternate splicing results in multiple transcript variants. [provided by RefSeq, Oct 2011]
*  Expression of T-type calcium current precedes neurite extension in neuroblastoma cells.
Abstract 1. N1E-115 mouse neuroblastoma cells morphologically differentiate by extending neurites in a period of seven days after addition of 2\% DMSO to the culture medium. We use..
*  Voltage-Activated Ca2+ Channels in Rat Renal Afferent and Efferent Myocytes: No Evidence for the T-Type Ca2+ Current.
AIMS: Based on indirect methods, it has been suggested that both L- and T-type Ca(2+) channels mediate signalling in the renal afferent arteriole and that T-type Ca channels are involved in signalling in the efferent arteriole. However, Ca(2+) curren
*  Plus it
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 Cav3.2 was sufficient to inhibit the growth, survival, and stemness of GSCs and also sensitized them to temozolomide chemotherapy. Proteomic and transcriptomic analyses revealed that Cav3.2 inhibition altered cancer signaling pathways and gene transcription. Cav3.2 inhibition suppressed GSC growth in part by inhibiting prosurvival AKT/mTOR pathways and stimulating proapoptotic survivin and BAX ...
*  "NMP-7 inhibits chronic inflammatory and neuropathic pain via block of " by N. Daniel Berger, Vinicius M. Gadotti et al.
Background: T-type calcium channels and cannabinoid receptors are known to play important roles in chronic pain, making them attractive therapeutic targets. We recently reported on the design, synthesis and analgesic properties of a novel T-type channel inhibitor (NMP-7), which also shows mixed agonist activity on CB1 and CB2 receptors in vitro. Here, we analyzed the analgesic effect of systemically delivered NMP-7 (intraperitoneal (i.p.) or intragstric (i.g.) routes) on mechanical hypersensitivity in inflammatory pain induced by Complete Freund's Adjuvant (CFA) and neuropathic pain induced by sciatic nerve injury.
*  Channelpedia
Jin-Yong Park, Ho-Won Kang, Hyung-Jo Moon, Sung-Un Huh, Seong-Woo Jeong, Nikolai M Soldatov, Jung-Ha Lee. J. Physiol. (Lond.), 2006 Dec 1 , 577, 513-23. T-type Ca2+ channels play essential roles in numerous cellular processes. Recently, we reported that phorbol-12-myristate-13-acetate (PMA) potently enhanced the current amplitude of Cav3.2 T-type channels reconstituted in Xenopus oocytes. Here, we have compared PMA modulation of the activities of Cav3.1, Cav3.2 and Cav3.3 channels, and have investigated the underlying mechanism. PMA augmented the current amplitudes of the three T-type channel isoforms, but the fold stimulations and time courses differed. The augmentation effects were not mimicked by 4alpha-PMA, an inactive stereoisomer of PMA, but were abolished by preincubation with protein kinase C (PKC) inhibitors, indicating that PMA augmented T-type channel currents via activation of ...
*  Plus it
T-type Ca2+ channels were originally called low-voltage-activated (LVA) channels because they can be activated by small depolarizations of the plasma membrane. In many neurons Ca2+ influx through LVA channels triggers low-threshold spikes, which in turn triggers a burst of action potentials mediated by Na+ channels. Burst firing is thought to play an important role in the synchronized activity of the thalamus observed in absence epilepsy, but may also underlie a wider range of thalamocortical dysrhythmias. In addition to a pacemaker role, Ca2+ entry via T-type channels can directly regulate intracellular Ca2+ concentrations, which is an important second messenger for a variety of cellular processes. Molecular cloning revealed the existence of three T-type channel genes. The deduced amino acid sequence shows a similar four-repeat structure to that found in ...
*  ICGenealogy - Channel: 102288-ICaT
Comments: T-type calcium channel, migliore file modified by m lazarewicz may 2001. Taken from lazarewicz et al. (2002), model no. 20007, with different implementation of kinetics. Functions hinf, minf, mtau and htau used in derivative states are replaced with procedure rates. Kinetics may be modified. Experimental results for im potassium current along with modeling. The animal model info here is from experimental results in the paper ...
*  Plus it
Although the biophysical properties of T-channels were first described in sensory neurons (Carbone and Lux, 1984), their function in nociception has only recently been established (Todorovic et al., 2001a; Bourinet et al., 2005; Choi et al., 2007). Indeed, the molecular mechanisms that regulate the function of these channels in pain processing still are not well understood. The major finding of this study is that LA inhibits native and recombinant T-currents by oxidizing specific thiol residues on the extracellular face of the channel. Inhibition of CaV3.2 T-channels and the ensuing decrease in cellular excitability in nociceptive DRG cells may contribute to the documented analgesic properties of LA in vivo. This notion is strongly supported by the finding that local intraplantar injection of LA potently diminished responses to noxious thermal and mechanical stimuli in wild-type mice, but was completely ineffective in CaV3.2 knock-out mice. ...
*  Participation of low-threshold calcium spikes in excitatory sy...
Participation of low-threshold calcium spikes in excitatory synaptic transmission in guinea pig medial frontal cortex.: We studied the activation of low-thresho
*  Reciprocal regulation of reactive oxygen species and phospho-CREB regulates voltage gated calcium channel expression during...
Sigma-Aldrich offers abstracts and full-text articles by [Arti Selvakumar, Cecil Antony, Jhalak Singhal, Brijendra K Tiwari, Yogendra Singh, Krishnamurthy Natarajan].
*  15pcs Plastic Plant T-type Tags Markers Seedling Nursery Gardening Stick Pink
The price of 15pcs Plastic Plant T-type Tags Markers Seedling Nursery Gardening Stick Pink is fair while it is also of high value. You can find whatever in you mind at a low price with free shipping at sourcingmap.
*  Genetic Models
Regulation of low-voltage activated T-type Ca2+ channel activity by kinases and heterotrimeric G-proteins and their roles in physiological responses.. ...