22 results about "Potassium channel" patented technology

The invention relates to potassium ion channel inhibitor compounds having improved affinity and selectivity for Kv1.3 ion channel, and enhanced stability. The inhibitor compounds comprise a polypeptide component which is a miniprotein. The invention also relates to therapeutic indications and diagnostic uses of the inhibitor compounds.

The invention discloses a non-sterilization type mildew-proof and antibacterial material capable of dynamically responding to thallus proliferation as well as a preparation method and application of the non-sterilization type mildew-proof and antibacterial material. The material comprises polyvinyl alcohol, carboxymethyl cellulose or a salt thereof and metal ions, and the polyvinyl alcohol, the carboxymethyl cellulose or the salt thereof are bridged through the metal ions; the metal ions comprise Li < + >. The material disclosed by the invention takes Na < + > released by thallus proliferation as a signal medium, releases Li < + > as required through a coordination-dissociation process, and further induces thallus cells to actively ingest Li < + > through metabolic deception of occupying a potassium ion channel by utilizing a hydration radius of Li < + > similar to K < + > according to the metabolic demand of sodium excretion and potassium ingestion in the thallus proliferation process; on one hand, bacterial cell replication lacks essential nutrient substance K < + >, and finally gradually declines; on the other hand, protein space conformation is changed and inactivated by capturing water molecules of intracellular protein, and the two aspects have a synergistic effect, so that the efficient mildew-proof and antibacterial effects of Li < + > at low concentration can be realized, and the effect is lasting.

The application discloses a KCR1 mutant suitable for plant potassium ion homeostasis regulation and application thereof, relates to the technical field of bioengineering, and the KCR1 mutant has at least T136A and G140A mutations on the basis of a light-controlled potassium ion channel protein KCR1. The application also discloses a gene encoding the KCR1 mutant. The application also discloses application of the KCR1 mutant or the gene in plant culture, breeding of new plant varieties or preparation of plant culture products. The KCR1 mutant has a blue-shifted excitation spectrum compared with a wild type, and can realize precise regulation of plant potassium ion flow through light regulation, and has great application value in light-controlled plant breeding and research of plant potassium ion channels.

This invention discloses US The application and methods of genes in regulating rice plant height, grain length, grain width, and grain weight belong to the field of crop genetics and breeding technology. This invention reveals for the first time the potassium ion channel protein gene. US This gene has a pleiotropic function in rice, regulating plant height, grain length, grain width, and grain weight. By silencing or knocking out this gene, rice plant height can be significantly reduced, lodging resistance can be enhanced, and grain length, grain width, and thousand-grain weight can be greatly increased. This overcomes the adverse effect of traditional dwarfing genes often being accompanied by smaller grains, achieving synergistic improvement in dwarfing and grain weight. The discovery of this gene provides a brand-new gene resource and an efficient molecular breeding target for high-yield, high-quality, and lodging-resistant rice breeding, and has important theoretical value and broad application prospects.

The invention belongs to the technical field of genetic engineering, and relates to a gene for regulating and controlling the potassium content of tobacco leaves, in particular to a tobacco potassium ion channel NtAKT1 gene and application thereof. The gene is a potassium ion channel, and the base sequence of the gene is as shown in SEQ ID NO. 1; wherein nucleotides from the 112th site to the 413th site are specific nucleic acid fragments. According to the invention, real-time PCR (polymerase chain reaction) shows that the gene has the highest expression quantity at the root of the tobacco. After a gene transient silencing technology (VIGS) or NtAKT1 gene knockout, the potassium ion content of tobacco leaves is remarkably reduced compared with that of a control group. According to the invention, the transport function of the NtAKT1 gene on the potassium content of the tobacco leaves is defined, a new evidence is provided for analyzing a molecular regulation mechanism of the potassium ion content of the tobacco leaves, a new thought is provided for regulating and cultivating high-potassium-content tobacco leaves through gene expression, and a new gene resource is provided for improving the potassium content of the tobacco leaves through a molecular means.

The invention provides a compound (I) or pharmaceutically acceptable salts and esters thereof, and a pharmaceutical composition containing the compound, and also provides application of the compound as a potassium ion channel regulator, application of the compound in preparation of drugs for potassium ion channel related diseases, and a corresponding pharmaceutical composition.

Disclosed is a compound of formula (I), wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds and methods of using the compounds to prevent and / or treat disorders associated with dysregulation of TREK-1, TREK-2 or both TREK-1 and TREK-2 in a mammal.

The invention relates to a polysubstituted aryl derivative, a preparation method of the polysubstituted aryl derivative and application of a pharmaceutical composition containing the polysubstituted aryl derivative in medicine. Specifically, the invention relates to a polysubstituted aryl derivative as shown in a general formula (I), a preparation method and a medicinal salt thereof, and application of the polysubstituted aryl derivative as a therapeutic agent, especially as a Kv1.3 potassium channel inhibitor, and definition of each substituent in the general formula (I) is the same as that in the specification.

The invention discloses a synergistic composition containing isoxazoline insecticidal and acaricide, which is composed of a compound I and a compound II, the compound I is CCXN-15-005-S (S configuration) or an agrochemically acceptable salt thereof, and the compound II is CCXN-15-005-S (S configuration) or an agrochemically acceptable salt thereof. The compound II is selected from any one of a nicotinic acetylcholine receptor agonist, a chordinal TRPV channel regulator, an acetyl-coenzyme A carboxylase (ACCase) inhibitor, a mitochondrial electron transfer inhibitor, a calcium-activated potassium ion channel regulator and trifluoroethyl thioether (sulfoxide) or an agrochemically acceptable salt thereof. The synergistic composition can be used for preventing and treating pests and harmful mites of thysanoptera, hemiptera and acarus and has a wider agricultural application prospect.

Disclosed is a compound of formula (I): Also disclosed are pharmaceutical compositions comprising the compound, methods of making the compound, kits comprising the compound and method of using the compound to prevent and / or treat disorders associated with dysregulation of TREK-1, TREK-2 or both TREK-1 and TREK-2 in a mammal.

The present application relates to a method for inhibiting neuronal hyperexcitability via AAV-mediated expression of a potassium channel. The present application relates to a recombinant adeno-associated virus vector (rAAV vector) for inhibiting neuronal hyperexcitability. The rAAV vector comprises a nucleotide sequence encoding a potassium channel. Further, the present application also relates to a virus particle comprising the rAAA vector, a pharmaceutical composition comprising the rAAA vector and / or the virus particle, and a use thereof in the preparation of a drug for treating diseases related to neuronal hyperexcitability.

This invention discloses a traditional Chinese medicine composition for regulating calcium ion homeostasis in the stomach, belonging to the field of traditional Chinese medicine technology. It is made from calcined oyster shell, calcined abalone shell, dried plum, poria cocos, and jujube seed in a specific weight ratio. This invention selects highly efficient calcium sources, calcined oyster shell and calcined abalone shell, in equal proportions, avoiding the deficiency of insufficient calcium content in traditional calcined dragon bone. It targets and supplements local calcium ions in the stomach, enhances the stabilizing effect of calcium ions on potassium ion channels, inhibits abnormal potassium ion leakage, and improves gastrointestinal smooth muscle tone. At the same time, it eliminates unsuitable medicinal materials such as Codonopsis pilosula, Astragalus membranaceus, Eucommia ulmoides, and Lycium barbarum. It uses Prunus mume to inhibit the proliferation of harmful bacteria in the small intestine and reduce fermentation and gas production, Poria cocos to supplement gastrointestinal trace elements, and Ziziphus jujuba var. spinosa to stabilize potassium ion channels, restore the calcium-potassium ion balance in the stomach, improve gastrointestinal motility rhythm, and alleviate problems such as small intestinal bacterial overgrowth, insufficient gastrointestinal motility, and abdominal distension. This composition does not contain sucrose, maltodextrin, chemical additives, or irritating excipients. It is fully decocted and suitable for people with fragile gastrointestinal barriers and immune sensitivity. The raw materials are safe and readily available, the preparation method is simple, and it has broad application prospects in gastrointestinal conditioning.

The application discloses an antiepileptic preparation preparation method and application of a micro ribonucleic acid 145b targeting agent, and relates to the technical field of biological medicine. The method comprises the following steps: constructing a neuron-specific recombinant adeno-associated virus plasmid vector, wherein the vector comprises a neuron-specific promoter hSyn, a reporter gene, an enhancer, and a functional nucleic acid sequence for targeting and inhibiting micro ribonucleic acid 145b; using an adeno-associated virus packaging system to transfect the vector to a packaging cell for virus packaging; collecting a lysis solution and separating out a recombinant adeno-associated virus particle through a purification process; and resuspending the virus particle to obtain a preparation. The application specifically down-regulates the miR-145b level in hippocampal neurons, releases the inhibition of the Kcnq3 potassium ion channel, further up-regulates the Kcnq3 expression, restores the M current, and reduces the neuron excitability from a molecular mechanism.

The present invention relates to a 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole derivative, a preparation method therefor, and a medical use of a pharmaceutical composition containing the derivative. Specifically, the present invention relates to a 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole derivative as shown in general formula (I), a preparation method therefor, and a pharmaceutically acceptable salt thereof, as well as a use thereof as a therapeutic agent, particularly as a Kv1.3 potassium channel inhibitor. The definitions of the substituents in general formula (I) are the same as those defined in the description.

The present invention addresses the problem of providing a new ischemic disease treatment strategy targeting pericytes. As a solution, the present invention provides an inflammation suppressant or a tissue protective agent for ischemic injury, each including an inhibitor which blocks ATP-sensitive potassium (KATP) channels present in a pericyte. In particular, the KATP channel is composed of pore-forming KIR6.1 and regulatory SUR2 subunits, and it is preferable for the inhibitor to act on the KIR6.1. The inflammation suppressant or the tissue protective agent for ischemic injury is preferably used in the treatment of ischemic diseases such as cerebral infarction or ischemic cardiac disease.

The invention belongs to the technical field of biomedicine, and particularly relates to a KV1.3 expression vector, a cell-free expression system, a recombination channel and application thereof. The recombinant expression vector is obtained by inserting a DNA (deoxyribonucleic acid) sequence as shown in SEQ ID NO.1 between an Nde I site and an Xho I site of a pIVEX-2. 4d vector, and the recombinant expression vector is named as pIVEX-K. The cell-free expression system is obtained by transferring the expression vector into a cell-free system. The recombination channel is obtained by recombining a cell-free expression system product and lipidosome. The recombinant channel can be applied to high-throughput screening of compounds influencing the potassium ion channel function, the influence of the compounds on the potassium channel function is directly displayed by monitoring the change of a fluorescence signal before and after a to-be-detected object is added, and the recombinant channel has the characteristics of simplicity in operation, short test period and high sensitivity.

The present invention provides the following compound (I) or a pharmaceutically acceptable salt and ester thereof, and a pharmaceutical composition comprising the compound of the present invention. The present invention further provides a use of the compound of the present invention as a potassium ion channel modulator, a use of the compound in the preparation of a drug for diseases related to potassium ion channels, and a corresponding pharmaceutical composition.

The invention belongs to the technical field of biological medicine, and particularly relates to preparation of a novel high-selectivity KV7.2 opener and application of the novel high-selectivity KV7.2 opener in antiepileptic drugs. A series of KV7.2-targeted small-molecule inhibitors are designed and synthesized, and the small-molecule inhibitors can enhance the current of a potassium ion channel KV7.2, accelerate channel activation and delay the inactivation process of the channel. The small molecule has a remarkable potential for treating epilepsy, shows efficient anti-epileptic activity in three classic epilepsy models for simulating human comprehensive attack and drug-refractory focal attack, is remarkably superior to positive control RTG, can be used for preparing anti-epileptic drugs and has a wide application prospect.

This disclosure relates to a benzothiazole derivative of formula (I) or a pharmaceutically acceptable salt thereof, its tautomers or stereoisomers thereof, methods of preparation and uses thereof, and pharmaceutical compositions thereof. It also provides the use of the compounds of the present invention as TREK-1 potassium channel modulators, and their use in alleviating and / or eliminating neuropsychiatric disorders. Furthermore, it provides the use of the compounds of the present invention in the preparation of medicaments for neuropsychiatric disorders. The present invention also provides treatment methods for diseases related to TREK-1 potassium channels.

Provided are an aryl tricyclic derivative, a preparation method therefor, and a use of a pharmaceutical composition containing the derivative in medicine. Specifically, provided are an aryl tricyclic derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof, and a use of the aryl tricyclic derivative and the pharmaceutically acceptable salt as a therapeutic agent, especially as a Kv1.3 potassium ion channel inhibitor, wherein the definition of each substituent in general formula (I) is the same as that in the description.

Compound of formula (I): JPEG2026521154000134.jpg4544 (wherein all symbols are defined herein) is disclosed. Also disclosed are pharmaceutical compositions comprising the compound, methods for preparing the compound, kits comprising the compound, and methods for using the compound to prevent and / or treat disorders associated with dysregulation of TREK-1, TREK-2, or both TREK-1 and TREK-2 in mammals.

The application discloses a kind of dynamic response bacteria proliferation non-sterilization type mildewproof bacteriostatic material and preparation method and application thereof.The material includes: polyvinyl alcohol, carboxymethyl cellulose or its salt, and metal ion, polyvinyl alcohol, carboxymethyl cellulose or its salt is bridged by metal ion;Metal ion includes Li + The material of the application releases Na + As signal medium by bacteria proliferation, through coordination-dissociation process, release Li + According to demand, further through the metabolic demand of sodium discharge and potassium absorption in the process of bacteria proliferation, utilize Li + With K + Similar hydrated radius, to occupy the "metabolic deception" of potassium ion channel, induce bacteria cell to actively absorb Li + On the one hand, lead to bacteria cell replication lack essential nutrient K + , finally gradually decline;On the other hand, by taking water molecules of intracellular protein, lead to protein spatial conformation change and inactivation, two aspects synergistic effect, realized Li + At low concentration, can high-efficiency mildewproof antibacterial, and the effect is durable.