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50 results about "L-type calcium channel" patented technology

The L-type calcium channel (also known as the dihydropyridine channel, or DHP channel) is part of the high-voltage activated family of voltage-dependent calcium channel. "L" stands for long-lasting referring to the length of activation. This channel has four subunits (Cav1.1, Cav1.2, Cav1.3, Cav1.4).

Compositions and methods of treatment using L-type calcium channel blockers and cholinesterase inhibitors

The present invention relates to compositions comprising at least one L-type calcium channel blocker, particularly the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, in combination with at least one cholinesterase inhibitor, particularly donepezil, and uses thereof in methods of treatment.
Owner:MEMORY PHARMA CORP

Treating stroke and other diseases without inhibiting N-type calcium channels

The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
Owner:NONO INC

Heterocycle amide t-type calcium channel antagonists

The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
Owner:BARROW JAMES C +3

Methods for screening compounds for proarrhythmic risk and antiarrhythmic efficacy

Methods for screening compounds for their potential to induce or inhibit a cardiac arrhythmia are disclosed. The methods comprise determining the ratio of the time constant (τ) of ICa,L recovery in tissue expressing the L-type calcium channel or any subunit or combination thereof of the L-type calcium channel treated with a test compound to the ventricular repolarization time of cardiac tissue treated with a test compound. The methods further comprise determining an arrhythmic risk score for a specified dose of a test compound.
Owner:MAIN LINE HEALTH HEART CENT

Derivatives of 1-phenoxy propan-2-ol and pharmaceutical composition containing the same

The present invention relates to a novel phenoxypropanol derivative, use thereof for blocking T-type calcium channel and / or TREK channel, and use thereof for preventing and / or treating T-type calcium channel- and / or TREK channel-associated diseases.
Owner:KOREA INST OF SCI & TECH

Method for recording T type calcium channel current by separating and cultivating newborn rat cortical neural cells

The invention provides a method for recording T type calcium channel current by separating and cultivating newborn rat cortical neural cells, and stably cultivated newborn rat cortical neural cells have a normal T type calcium ion channel function. The method is suitable to research on the physiological and pharmacological characteristics of the rat cortical neural cells by a patch clamp technique. The experiment operation is easy to master, and the method for stably cultivating the separated newborn rat cortical neural cells is simple and efficient. The success rate, the stability and the repeatability of an experiment are increased apparently by means of stably cultivating the separated newborn rat cortical neural cells.
Owner:辉源生物科技(上海)有限公司

Design and application of gene coding calcium probe GCaMP-X

ActiveCN107987171AReduce the impactChanges in the real objective concentrationCompound screeningApoptosis detectionNitrogenExcitation transcription coupling
The invention discloses an optimized and improved gene coding calcium probe GCaMP-X and basic application thereof. The probe comprises a GCaMP protein, a first amino acid sequence and a second amino acid sequence, wherein the first amino acid sequence refers to fragments capable of weakening pre-binding capacity between calmodulin un-bound with calcium ions and an L type calcium channel (LTCC); the second amino acid sequence is a localization sequence (intranuclear, extranuclear and other subcellular regions); the first amino acid sequence is located at a nitrogen terminal of the GCaMP protein; and the second amino acid sequence is located at a carbon terminal of the GCaMP protein. Compared with each kind of the conventional GCaMP probes, the optimized GCaMP-X probe has effects of eliminating interference effects on nerve cell LTCC and mediated excitation-transcription coupling thereof and objectively and accurately measuring calcium signals of nerve cells.
Owner:TSINGHUA UNIV

Mice lacking alpha 1g showing enhanced novelty-seeking and alcohol preference and therapeutic methods for mood disorders by modulating alpha 1g t-type calcium channels

The present invention relates to a novel use of an α1G T-type calcium channel transgenic mouse as a nervous disease model, more particularly, a novel use of a mouse deficient in α1G T-type calcium channel showing novelty-seeking and alcohol preference as a nervous disease model for human nervous related diseases such as novelty-seeking character, alcoholism, anxiety and emotion disorder by stress, etc. The α1G T-type channel transgenic mice showing novelty-seeking and alcohol preference of the present invention can be effectively used for the development of a medicine and a therapeutic method for human nervous diseases.
Owner:KOREA INST OF SCI & TECH

Method for the prevention and treatment of essential tremor by regulating alpha1g t-type calcium channel or by t-type calcium channel blockers

The present invention relates to a method for the prevention and treatment of essential tremor by blocking α1G T-type calcium channel, a preventive and therapeutic agent for essential tremor containing the α1G T-type calcium channel blocker as an active ingredient, and a screening method of a preventive and therapeutic agent for essential tremor by investigating α1G T-type calcium channel blocking activity. More precisely, the present invention relates to a method for the prevention and treatment of essential tremor by using α1G T-type calcium channel blocker, for which the inventors confirmed that the α1G T-type calcium channel knock out mice (α1G − / −) had resistance against essential tremor and when the T-type channel blocker was administered to the wild type mice (α1G + / +), they gained resistance against essential tremor.
Owner:KOREA ADVANCED INST OF SCI & TECH

T Type Calcium Channel Inhibitors

The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels,whereinR1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;Z is NH, NCH3, O, S, or CH2;Y is NH, O, or CH2 with the proviso that Y and Z are not the same;R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; andR3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.
Owner:UNIV OF VIRGINIA ALUMNI PATENTS FOUND

Methods for identifying agonists and antagonists of human T-type calcium channels

Sequences and partial sequences for three types of mammalian (human and rat) sequences identified) T-type calcium channel subunits which we have labeled as the α1G, α1H and α1I subunits are provided. Knowledge of the sequence of these calcium channel permits the localization and recovery of the complete sequence from human cells, and the development of cell lines which express the novel calcium channels of the invention. These cells may be used for identifying compounds capable of acting as agonists or antagonists to the calcium channels.
Owner:ZALICUS PHARMA LTD (CA)

Methods for screening compounds for proarrhythmic risk and antiarrhythmic efficacy

Methods for screening compounds for their potential to induce or inhibit a cardiac arrhythmia are disclosed. The methods comprise determining the ratio of the time constant (τ) of ICa,L recovery in tissue expressing the L-type calcium channel or any subunit or combination thereof of the L-type calcium channel treated with a test compound to the ventricular repolarization time of cardiac tissue treated with a test compound. The methods further comprise determining an arrhythmic risk score for a specified dose of a test compound.
Owner:MAIN LINE HEALTH HEART CENT

T type calcium channel blockers and the treatment of diseases

The present invention provides a method for treating a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, which comprises administering to the mammal a therapeutically effective amount of a T type calcium channel inhibitor, a prodrug thereof, or a pharmaceutically acceptable salt of said inhibitor or prodrug, wherein the T type calcium channel inhibitor blocks a splice variant of an α1H isoform of T type calcium channels.
Owner:UNIV OF VIRGINIA ALUMNI PATENTS FOUND

Method for recording L type calcium channel current by separating guinea pig ventricular muscle cells

An L type calcium channel is mainly distributed in heart, blood vessels, endocrine and nervous systems, and plays a vitally important role in heart and smooth muscle excitation-contraction coupling, atrionector and atrioventricular node action potential conduction. The method that the influence of a compound on the L type calcium channel is observed through a patch clamp recording method so as to evaluate a hearth safety coefficient of the compound and the effect of treating the hypertension becomes an important research mode. According to the method for recording the L type calcium channel current by separating the guinea pig ventricular muscle cells, through improving a perfusate storage mode, the yield rate and the survival rate of separating the guinea pig ventricular muscle cells are increased, and the stabilization time of the cells is prolonged, and thus the success rate and the stability of experiments are increased.
Owner:辉源生物科技(上海)有限公司

Ion Channel Inhibitory Compounds, Pharmaceutical Formulations, and Uses

The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and / or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.
Owner:AFASCI

CANINE iPS CELLS AND METHOD OF PRODUCING SAME

InactiveUS20110033936A1Stable productionEffectively utilizableGenetically modified cellsCell culture active agentsMitogen-Activated Protein Kinase Kinase InhibitorA-DNA
Provided are a method of producing canine iPS cells, comprising (a) the step of bringing into contact with each other a canine somatic cell and a nuclear reprogramming factor, and (b) the step of culturing the cell in a medium containing at least one substance selected from the group consisting of a mitogen-activated protein kinase kinase inhibitor, an activin receptor-like kinase inhibitor, a glycogen synthase kinase inhibitor, a L-type calcium channel agonist and a DNA methylation inhibitor, and a leukemia inhibitory factor, and canine iPS cells that can be obtained by the method.
Owner:KYOTO UNIV

Omega conotoxins

The present invention relates to a method for increasing the binding reversibility of a ω-conotoxin to a N-type calcium channel, which comprises preparing a ω-conotoxin having a Ile and / or Ala residue at a position of amino acid (11 and / or 12), respectively in the second loop between cysteine residues (2 and 3) of the ω-conotoxin represented by the formula I, such that the prepared ω-conotoxin has the increased binding reversibility to N-type calcium channel. In addition, the present invention relates to a novel ω-conotoxin and a pharmaceutical composition having plausible properties in view of blocking activity to and specificity to N-type calcium channel, and dramatically improved binding reversibility to N-type calcium channel.
Owner:ANYGEN

Preventing Arrhythmias Associated with Cell Transplantation

Skeletal myoblasts are an attractive cell type for transplantation since they are autologous and resistant to ischemia. However, clinical trials of myoblasts transplantation in heart failure have been plagued by ventricular tachy-arrhythmias and sudden cardiac death. The pathogenesis of these arrhythmias is poorly understood, but may be related to the fact that skeletal muscle cells, unlike heart cells, are electrically isolated by the absence of gap junctions. An in vitro model of myoblasts transplantation into cardiomyocyte monolayers can be used to investigate the mechanisms of transplant-associated arrhythmias. Co-cultures of human skeletal myoblasts and rat cardiomyocytes result in reentrant arrhythmias (spiral waves) that reproduce the features of ventricular tachycardia seen in patients receiving myoblasts transplants. These arrhythmias can be terminated by nitrendipine, an L-type calcium channel Mocker, but not by the Na channel blocker lidocaine. Genetic modification of myoblasts to stably express the gap junction protein connexin 43 decreases arrhythmogenicity in co-cultures. It similarly can be used to increase the safety of myoblasts transplantation in patients.
Owner:THE JOHN HOPKINS UNIV SCHOOL OF MEDICINE

Methods of using proteinacious channels to identify pharmaceutical treatments and risks, and treatments resulting therefrom

Methods and therapeutic strategies utilizing proteinacious channels in lipid membranes of mammalian cells. The methods entail administering a pharmaceutical to a lipid membrane of a mammalian cell, and then determining the effect of the pharmaceutical on the electrophysiology of at least one proteinacious channel of the lipid membrane, wherein the proteinacious channel is a Kv7 potassium channel and / or a L-type calcium channel of an airway smooth muscle cell (ASMC). The method can be used to identify pharmaceuticals that may be used to treat asthmatic and other bronchospastic conditions that can lead to airway obstruction, or to perform drug screening to assess potential risk of pharmaceuticals.
Owner:LOYOLA UNIV OF CHICAGO

4-fluoro-piperidine T-type calcium channel antagonists

The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
Owner:MERCK SHARP & DOHME LLC

Compositions for Increasing Hair Growth

Cosmetic skin and hair care compositions for enhancing the growth and appearance of mammalian hair in an individual are provided, which compositions comprise a dose of an L-type calcium channel blocker effective to promote anagen phase of the hair cycle. As shown herein, anagen phase promotion can result in more rapid hair growth.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV

Heterocycle amide t-type calcium channel antagonists

The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
Owner:MERCK SHARP & DOHME LLC

T type calcium channel inhibitors

The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels,whereinR1 is C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;Z is NH, NCH3, O, S, or CH2;Y is NH, O, or CH2 with the proviso that Y and Z are not the same;R2 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy;m and n are independently selected from integers ranging from 1-5 with the proviso that m+n=an integer ranging from 2-9; andR3 is H, halo, NH2, C1-C4 alkyl, hydroxy, or C1-C4 alkoxy.
Owner:UNIV OF VIRGINIA ALUMNI PATENTS FOUND
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