13 results about "Channel blocker" patented technology

This invention provides a method for improving the antidepressant effect of an NMDAR pore channel blocker, comprising: (1) performing behavioral, pharmacological, or physical measures before or during the plasma half-life of the NMDAR pore channel blocker to open ion channels of a larger proportion of NMDAR molecules in the lateral habenula (LHb); and optionally (2) performing behavioral, pharmacological, or physical measures after administration of the NMDAR pore channel blocker to prevent or reduce the dissociation of NMDAR pore channel blocker molecules from NMDAR. Treatment regimens and drug combinations for effectively treating depression are also provided. This disclosure further provides a drug delivery system comprising an implantable unit capable of controlled, repeatable, and precise in vivo delivery of an NMDAR pore channel blocker, as well as an initiator and / or enhancer, to an LHb region of a subject's brain, thereby achieving improved therapeutic effects.

The present invention is related to methods of treating cardiac arrhythmia, angina, or a migraine in a patient in need thereof, with a therapeutically effective amount of a compound having a structure according to the formula:the method comprising nasally administering to the patient (i) a first dose, and (ii) a second dose of an aqueous composition comprising a pharmaceutically acceptable acetate or methanesulfonate salt of compound I, or a racemate or enantiomer thereof, wherein the acetate or methanesulfonate salt of compound I, or the racemate or enantiomer thereof, is dissolved in the aqueous composition at a concentration of 350 mg / mL±50 mg / mL, and wherein the second dose of the compound is administered between 5 minutes and 25 minutes after the first dose.

Provided are a tetrodotoxin conjugate, a method for preparing same, and use thereof. A carboxyl-containing macromolecular compound and tetrodotoxin are used as the starting materials, and after a catalyst and a solvent are added, the tetrodotoxin conjugate is obtained by means of a coupling reaction. The carboxyl-containing macromolecular compound is selected from carboxylated dextran, carboxylated β-cyclodextrin, alginic acid, and polyacrylic acid. The tetrodotoxin conjugate can be used in the preparation of a sodium channel blocker and a medicament for treating neuropathic pain caused by chemotherapy, and possesses an analgesic effect associated with tetrodotoxin (TTX). In addition, the therapeutic window is increased, thereby greatly improving the safety.

The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.

An insecticidal composition containing cybenzoxasulfyl and the use thereof. The insecticidal composition contains active ingredient A and active ingredient B, wherein active ingredient A is cybenzoxasulfyl, and active ingredient B is selected from one or more of the following compounds: an acetylcholinesterase inhibitor, a nicotinic acetylcholine receptor (nAChR) channel blocker, nicotinic acetylcholine receptor (nAChR) allosteric modulator site I, a nicotinic acetylcholine receptor (nAChR) competitive modulator, a glutamate-gated chloride channel (GluCl) allosteric modulator, etc. The composition has reasonable components, good insecticidal effects, and low administration costs, and also has the characteristics of a reduced application amount, safety to crops, reduced pesticide residues, etc.

The invention discloses an external eye protection liquid for relieving asthenopia and a preparation method thereof.The eye protection liquid comprises a plant-derived calcium channel blocker, a divalent metal ion source, a temperature-sensitive gel matrix and a deep eutectic solvent system, has unique reversible phase change characteristics, is flowing sol during low-temperature storage, and can be used for relieving asthenopia. And after contacting the ocular surface, in-situ phase change is rapidly generated to form semi-solid gel. In the preparation process, a choline chloride-propylene glycol deep eutectic solvent is adopted to carry out low-temperature in-situ extraction on plant raw materials, an extracting solution is directly used as a functional component to be reserved in the preparation, and a cold-soluble compounding process of a poloxamer matrix is matched, so that the damage of high temperature to active components in the whole process is avoided. The problems that a traditional aqueous solution is short in retention time on the ocular surface and low in bioavailability, and the drug effect is damaged by a high-temperature process are solved, and deep eyestrain is effectively relieved through physical and physiological dual mechanisms.

An insecticidal composition containing oxazosulfyl and a use thereof, relating to the technical field of pesticides. The insecticidal composition comprises an active ingredient A and an active ingredient B, wherein the active ingredient A is oxazosulfyl; and the active ingredient B is selected from one or more of the following compounds: an acetylcholinesterase inhibitor, a nicotinic acetylcholine receptor (nAChR) channel blocker, an nAChR allosteric modulator site I, an nAChR competitive modulator, a glutamate-gated chloride channel (GluCl) allosteric modulator, etc. The composition has a reasonable formulation, good insecticidal efficacy, and low application costs, and has the characteristics of reduced application amount, safety to crops, reduced pesticide residue, etc.

The present disclosure relates to methods and pharmaceutical compositions of angiotensin converting enzyme inhibitor and calcium channel blocker, particularly stable oral liquid compositions including angiotensin converting enzyme inhibitor, calcium channel blocker and one or more pharmaceutically acceptable excipients for the treatment of hypertension, coronary artery disease, heart failure, acute myocardial infarction and other related cardiovascular diseases.

The present invention relates to a synergistic pesticidal composition for controlling pest infection in plants, more particularly to a synergistic composition comprising at least three active ingredients selected from (I) a mitochondrial complex I electron transport inhibitor selected from Tolfenpyrad; (II) acetyl-CoA carboxylase inhibitor selected from Spidoxamat, Spirodiclofen, Spiromesifen, Spiropidion, and Spirotetramat; and (III)nicotinic acetylcholine receptor (nAChR) channel blocker is selected as Thiocyclam Hydrogen Oxalate. The invention further relates to a process of preparing said composition along with one or more inactive excipient and formulation thereof. The composition overcomes the pest infestations much more efficiently and provides the advantages of overcoming the resistance of the pest to the use of the individual components of the pesticide composition, improved shelf life, increased spectrum of activity, better crop quality, enhanced efficacy, and economic and ecological advantages i.e. more yield, less expensive and environmentally safe composition.

The present disclosure relates to methods and pharmaceutical compositions of angiotensin converting enzyme inhibitor and calcium channel blocker, particularly stable oral liquid compositions including angiotensin converting enzyme inhibitor, calcium channel blocker and one or more pharmaceutically acceptable excipients for the treatment of hypertension, coronary artery disease, heart failure, acute myocardial infarction and other related cardiovascular diseases.

A method and composition for modulating male fertility are disclosed, centered on the targeted alteration of transmembrane channel-like (TMC) protein function, activity, or gene expression. Small molecules or pharmaceutically acceptable salts or solvates thereof are provided to modulate the activity or expression of TMC proteins, such as TMC5, in testis tissue. The compositions may include TMC5 channel blockers, dimerization inhibitors, TMC5-CIB1 interaction inhibitors, or small interfering RNAs targeting TMC5 mRNA, optionally formulated with a pharmaceutically acceptable carrier and capable of crossing the blood-testis barrier. Methods of diagnosing male infertility are also provided, comprising quantitating TMC5 expression or activity and comparing to a standard to identify infertility. These approaches enable reversible, non-hormonal regulation of spermatogenesis and fertility, offering new therapeutic strategies for male contraception and infertility treatment.