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

Methods for modulating T-type calcium channel activity without directly targeting the T-type calcium channels are provided that include modulating kelch-like protein 1 (KLHL1) levels in a subject by providing a small hairpin RNA (shRNA) that targets a KLHL1 gene, and then administering the shRNA to the subject in an amount sufficient to modulate KLHL1 gene expression. The KLHL1 level directly effects current activity in T-type calcium channels and therefore modulation of KLHL 1 gene expression indirectly modulates current activity in T-type calcium channels. The methods may be implemented with, for example, an shRNA molecule suitable for modulating a KLHL1 level in the subject which may be provided as a plasmid encoding the shRNA molecule or an adeno-associated virus vector encoding the shRNA molecule. Methods of identifying compounds that modulate current activity in T-type calcium channels by determining an effect of the compound on KLHL1 gene expression are also provided.

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.

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.

The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the formula set forth below or its pharmaceutically acceptable salts, and its preparation method thereof.The compound of Formula 1 is a novel piperazinylalkylpyrazole derivative, which particulary has T-type Ca2+ channel blocking effect and thus can be useful as a therapeutic agent for nerve and muscle pain.

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.

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.

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.

Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and / or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament for the treatment of cardiovascular diseases, apoplexy or senile dementia are also disclosed in the present invention.

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.