72 results about "Calcium channel" patented technology

The invention relates to the use of cannabidiol (CBD), at a dose of greater than 300 mg / day, in combination with a standard anti-epileptic drug (SAED) which acts via sodium or calcium channels, for use in the treatment of epilepsy. The SAED is preferably one which •modities low-threshold or transient neuronal calcium currents, or •reduces high-frequency neuronal firing and sodium-dependent action potentials and enhances GABA effects. Preferred SAEDs are ethosuximide and valproate.

Described herein, in part, are methods useful for preventing and / or treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as psychiatric disorders (e.g., mood disorder (e.g., major depressive disorder)), pain, tremor (e.g., essential tremor), seizures (e.g., absence seizures), epilepsy, or an epilepsy syndrome (e.g., juvenile myoclonic epilepsy). The present invention further comprises methods for modulating the function of a T-type calcium channel and methods of administering a titrated dosage of a T-type calcium channel antagonist.

Described herein, in part, are methods useful for preventing and / or treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as Parkinson's disease, psychiatric disorders (e.g., mood disorder (e.g., major depressive disorder)), pain, tremor (e.g., essential tremor), seizures (e.g., absence seizures), epilepsy, or an epilepsy syndrome (e.g., juvenile myoclonic epilepsy). The present invention further comprises methods for modulating the function of a T-type calcium channel and methods of administering a titrated dosage of a T-type calcium channel antagonist.

The invention provides an application of two polycyclic polyisopentenyl acyl phloroglucinol compounds (PPAP) with different skeleton types in preparation of drugs for relieving / treating neurodegenerative diseases. Belongs to the technical field of medicines. Hypheronone A provided by the invention is a 1, 9-split-ring polycyclic polyisopentenyl phloroglucinol compound, and hypheronone L is a polycyclic polyisopentenyl phloroglucinol compound which is formed by carrying out intramolecular [4 + 2] cyclization on a monocyclic polyisopentenyl phloroglucinol compound and has a complex ring system. The compound hypherone A and the compound hypherone L both have the activity of enhancing the current of a voltage-gated T-type calcium channel, can be used for preparing medicines for treating neurodegenerative diseases, particularly can be used for preparing medicines for relieving and / or treating diseases such as spinal cerebellar ataxia, Alzheimer's disease and intellectual syndrome, and have clinical application value.

Disclosed herein are compounds for treating a condition modulated by calcium channel ion activity and pharmaceutical compositions comprising the compounds, wherein the compounds comprise a diazaspiroheptane core and left- and right-hand substitutions of the diazaspiroheptane core. Also disclosed herein are methods using the compounds to treat a disease or condition relating to aberrant function or activity of a T-type calcium channel.

Described herein are T-type voltage-gated calcium channel enhancers capable of enhancing thalamic function, e.g., reducing thalamic cortex hyperactivity in a patient in need thereof. These enhancers may be useful for many diseases or conditions associated therewith, such as schizophrenia and neurodevelopmental disorders. The CaV enhancers typically have a structure of formula (I) or formula (V). # imgabs0 #

The present disclosure provides a cell patch cryopreservation solution, which includes: a cryoprotectant, a buffer, a reducing agent, a calcium channel inhibitor and an apoptosis inhibitor. The present disclosure also provides a method of cryopreserving a cell patch by using the aforementioned cell patch cryopreservation solution. The cell patch cryopreservation solution and the method of cryopreserving a cell patch provided by the present disclosure can maintain the structural integrity and the cell activity of the cell patch.

The invention discloses a polysubstituted cyclopropyl carbonyl compound with calcium ion channel regulation activity as well as a pharmaceutical composition and application thereof, and belongs to the technical field of medicines. An alpha-chlorocyclobutanone compound is used as a raw material and reacts with aryl magnesium bromide with different substituent groups in an organic solvent, and the polysubstituted cyclopropyl carbonyl compound is obtained in one step. The polysubstituted cyclopropyl carbonyl compound is novel in structure, the preparation method has the advantages of being low in cost, simple and convenient to operate, mild in condition and the like, and the polysubstituted cyclopropyl carbonyl compound novel in structure can be rapidly obtained. The prepared cyclopropyl carbonyl compound has T-type calcium channel regulation activity and has an analgesic effect.

The application belongs to the field of heart disease treatment and natural medicine compound, and provides application of bufalin or a pharmaceutically acceptable salt thereof in preparation of a medicine for treating reperfusion arrhythmia. Experiments in vitro and in vivo prove that bufalin inhibits L-type calcium channels in a concentration-dependent manner, reduces extracellular calcium ion inflow, and further reduces the incidence of ventricular arrhythmia, arrhythmia, reduces ventricular conduction time, increases left ventricular conduction velocity, and reduces ventricular conduction dispersion; and provides a new drug selection for the treatment of reperfusion arrhythmia.

Described herein, in part, are single-unit dosage forms, comprising the compound of Formula (I) or a pharmaceutically acceptable salt thereof (e.g., the compound of Formula (II), e.g., PRAX-944 HCl), wherein the composition is bioequivalent to a reference composition of the same dosage strength administered as multiple small, round tablets. The present invention further comprises methods useful for treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as tremor (e.g., essential tremor).

To provide dosage forms and compositions useful for preventing and / or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)).SOLUTION: Provided is an oral dosage form comprising: a compound of the following formula or a pharmaceutically acceptable salt thereof; and a modified-release polymer.SELECTED DRAWING: None

The present application provides a method for regulating calcium ion influx of myocardial cells by modifying any one or more of the amino acid residues in the combination of ESSE at positions 2061-2064 in the amino acid sequence corresponding to SEQ ID No. 1 of the mammalian L-type calcium channel protein, and a calcium channel regulator. The present application also provides a pharmaceutical composition for treating cardiovascular diseases, which comprises a regulator of any one or more of the amino acid residues in the combination of ESSE at positions 2061-2064 in the amino acid sequence corresponding to SEQ ID No. 1 of the mammalian L-type calcium channel protein. The present application also provides a method for screening potential substances for treating cardiovascular diseases.

The present disclosure provides a crystalline form of Form D, i.e., a N-((1-(2-(tert-butylamino)-2-oxoethyl) piperidin-4-yl) methyl)-3-chloro-5-fluorobenzamide hydrochloride trihydrate (Compound 1). The disclosure also provides pharmaceutical compositions comprising Compound 1 in Form D, and methods of treating neurological and psychiatric disorders by administering Compound 1 in Form D or a pharmaceutical composition comprising Compound 1 in Form D to a subject in need thereof.

This invention discloses bridged tricyclic γ-aminobutyric acid (GABA) derivatives targeting the α2δ subunit of voltage-gated calcium channels. These compounds exhibit enhanced binding affinity and improved pharmacological profiles. They aim to overcome limitations of current α2δ ligands like gabapentin and pregabalin. The new derivatives show potential for treating neuropathic pain, epilepsy, and related disorders.

Described herein, in part, are methods useful for treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as essential tremor, in a subject in need thereof, comprising administering a T-type calcium channel inhibitor in combination with at least one of propranolol, primidone, topiramate, or a pharmaceutically acceptable salt thereof. Also disclosed herein are compositions comprising the T-type calcium channel inhibitor and at least one of propranolol, primidone, topiramate, or a pharmaceutically acceptable salt thereof.

The invention discloses a method for up-regulating L-type calcium channels of myocardial cells, and belongs to the technical field of molecular biology. In order to solve the problem that a method for up-regulating the L-type calcium channel of the myocardial cell with high safety and high efficiency is lacked in the prior art, the invention provides a method for up-regulating the L-type calcium channel of the myocardial cell by combining in-vivo intravenous injection or in-vitro direct incubation of a sound-sensitive agent with low-frequency and low-intensity ultrasonic irradiation treatment. According to the method for up-regulating the L-type calcium channel of the myocardial cell, the L-type calcium channel of the myocardial cell can be up-regulated, the percentage and frequency of spontaneous atrial fibrillation of a rabbit with atrial fibrillation can be reduced, the atrial fibrillation induction rate can be reduced, the effective atrial refractory period can be prolonged, the action potential time history of acute separation rabbit atrial muscle cells can be prolonged, and the current density of the L-type calcium channel of the atrial muscle cells can be increased; and mRNA and protein expression of the L-type calcium channel pore forming subunit CACNA1C are increased.

The present disclosure provides Pattern D, i.e., a crystalline form of N-((1-(2-(tert-butylamino)-2-oxoethyl)piperidin-4-yl)methyl)-3-chloro-5-fluorobenzamide hydrochloride salt trihydrate (Compound 1). The present disclosure also provides pharmaceutical compositions comprising Compound 1 in the form of Pattern D, as well as methods of treating neurological and psychiatric disorders by administering to a subject in need thereof Compound 1 in the form of Pattern D or a pharmaceutical composition comprising Compound 1 in the form of Pattern D.

The present invention relates to homopiperazinyl and homopiperidinyl quinazolin-4(3H)-one derivatives having dual pharmacological activity towards both the α2δ subunit of the voltage-gated calcium channel and the sigma-1 (σ1) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

This disclosure relates to 1,4-oxazolidinyl heptane and 1,4-thioazolidinyl heptane derivatives, and their use in treating conditions and diseases associated with the lanodid receptor (RyR), which regulates calcium channel signaling in cells. This disclosure also discloses pharmaceutical compositions comprising these compounds and their use in treating diseases and conditions associated with RyR dysfunction, particularly cardiovascular, musculoskeletal, and central nervous system (CNS) disorders.

Provided herein are compositions and methods protection against QTc prolongation. In some embodiments, the compositions and methods comprise administering a compound having one or more of early sodium ion channel blocking, lates sodium ion channel blocking, and L-type calcium channel blocking activity. In some embodiments, the compound is sulcardine or a pharmaceutically acceptable salt thereof, such as sulcardine sulfate or sulcardine mono-edisylate.

A method of inducing expression of a calcium channel and / or a calcium pump in a cell includes: irradiating the cell with light in a wavelength range of 315-325 nm. The calcium channel and / or the calcium pump is / are at least one selected from the group consisting of dihydropyridine receptor (DHPR), voltage-gated calcium channel (VGCC), ryanodine receptor (RYR), and sarcoendoplasmic reticulum Ca2+-ATPase (SERCA).

The present invention concerns the use of an L-type calcium channel (LTCC) blocker in combination with a BRAF inhibitor (BRAFi) and / or a MEK inhibitor (MEKi) for the treatment of melanoma in a patient.

The present invention discloses the use of 4-chloro-3-ethylphenol in the preparation of drugs for preventing or treating ulcerative colitis and sepsis, and relates to the field of biomedical technology. It is experimentally confirmed in the present invention that the ryanodine receptor (RyRs) agonist 4-chloro-3-ethylphenol has significant effects in preventing or treating ulcerative colitis and sepsis, and 4-chloro-3-ethylphenol is a clinically potential drug for the preparation of drugs for preventing or treating ulcerative colitis and sepsis; meanwhile, using 4-chloro-3-ethylphenol as a reliable tool can clearly distinguish the two components of store-operated calcium channels (SOCE), that is, inducing ER / Ca<supgt;2+< / supgt; release through RyR, but blocking the entry of Ca<supgt;2+< / supgt; through SOC in vascular endothelial cells, having a dual effect; further experiments confirm that pure endothelial cell RyR / ER / Ca<supgt;2+< / supgt> release is a unique pathway for regulating EDH-mediated arterial vasodilation in a healthy state and has an anti-inflammatory effect on ulcerative colitis and sepsis.

Described herein, in part, are methods useful for preventing and / or treating a disease or condition relating to aberrant function or activity of a T-type calcium channel, such as psychiatric disorders (e.g., mood disorder (e.g., major depressive disorder)), pain, tremor (e.g., essential tremor), seizures (e.g., absence seizures), epilepsy, or an epilepsy syndrome (e.g., juvenile myoclonic epilepsy). The present invention further comprises methods for modulating the function of a T-type calcium channel and methods of administering a titrated dosage of a T-type calcium channel antagonist.

Described herein, in part, are dosage forms and compositions useful for the prevention and / or treatment of diseases or conditions associated with aberrant T-type calcium channel function, such as epilepsy and epileptic syndromes (e.g., absent seizures, teenager myospastic epilepsy or genetic epilepsy), tremor (e.g., epilepsy seizures, spasmodic epilepsy, or hereditary epilepsy), or tremor (e.g., epilepsy seizures). Idiopathic tremor (e.g., idiopathic tremor) and psychiatric disorders (e.g., mood disorders (e.g., severe depressive disorder)). The invention also includes methods for modulating the function of T-type calcium channels.

A pharmaceutical composition for use in the treatment or prevention of a disease or condition associated with a calcium release activated calcium (CRAC) channel or a disease or condition associated with discoid domain receptor 2 (DDR2) in an individual in need thereof. A pharmaceutical composition for inhibiting CRAC channel activity and / or DDR2 activity in cells of an individual. The pharmaceutical composition comprises an effective amount of at least one selected from the group consisting of WRG-28, atorvaquone (Av), a WRG-28 precursor, and an atorvaquone (Av) precursor, and a pharmaceutically acceptable carrier thereof.

Described herein, in part, are dosage forms and compositions useful for preventing and / or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel.

The present disclosure describes a method of reducing Miro1 and / or phosphorylated alpha-synuclein level in a cell, for example, by contacting the cell with an effective amount of a T-type calcium channel antagonist or a ferroptosis inhibitor.

The present invention is directed, in part, to deuterium-enriched compounds and compositions comprising deuterium-enriched compounds useful for preventing and / or treating diseases or conditions associated with abnormal function of T-type calcium channels. As described herein, deuteration of the T-type calcium channel inhibitors can significantly affect metabolic clearance. Surprisingly, some of the deuterated compounds described herein exhibit significantly improved metabolic stability compared to non-deuterated compounds. Because metabolic clearance often leads to improved bioavailability, deuterated compounds are expected to have improved bioavailability compared to non-deuterated compounds.