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

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.

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.

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.

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.

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.

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.

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.

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,

wherein

R₁ 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; and

R₃ is H, halo, NH₂, C₁-C₄ alkyl, hydroxy, or C₁-C₄ alkoxy.

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.

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.

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.

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.

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.

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.