35 results about "Sodium channel" patented technology

The invention relates to the field of biological medicine, in particular to a compound and a preparation method and application thereof. Particularly, the invention relates to a compound shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, solvate, isotope labeled compound or polymorphic substance thereof, a preparation method thereof, a pharmaceutical composition containing the compound and application thereof, the compound can be used as a sodion channel inhibitor, has an analgesic effect, and can be used for preparing a sodion channel inhibitor. The compounds of the present application also have a variety of excellent properties. # imgabs0 #

Small molecule inhibitors of Nav1.8 voltage-gated sodium ion channel, including compounds of formula (I), (II), (III), (IV), and (V) are described. Also described are pharmaceutical compositions containing a compound of formula (I), (II), (III), (IV), and (V) and uses of the compounds and pharmaceutical compositions for inhibiting Nav1.8 voltage-gated sodium channels and treating Nav1.8 mediated diseases, such as pain and pain-associated diseases and cardiovascular diseases, such as atrial fibrillation.

This invention discloses a rare-earth metal gradient-doped polyanionic cathode material, its preparation method, and its application. The molecular formula of the rare-earth metal gradient-doped polyanionic cathode material is Na. 2+2x‑y RE y Fe 2‑x (SO4)3, in the rare earth metal gradient-doped polyanionic cathode material, rare earth metal elements enter the crystal lattice of the polyanionic cathode material in the form of rare earth metal ions, and the doping content of the rare earth metal ions decreases in a gradient along the direction from the crystal lattice surface to the bulk phase. The polyanionic cathode material is an Alluaudite-type sodium iron sulfate cathode material. This invention effectively solves the kinetic mismatch problem of "fast ions but slow electrons" in rate performance by simultaneously optimizing the electronic structure and sodium ion channels through rare earth doping, significantly improving the structural stability of the material under long-cycle and fast-charge-discharge conditions. Simultaneously, the assembled sodium-ion battery exhibits excellent wide-temperature performance.

The invention relates to the field of solenopsis invicta prevention and control, in particular to a long-acting solenopsis invicta killing bait and a preparation method thereof.The long-acting solenopsis invicta killing bait is prepared from indoxacarb, sophocarpidine, huperzine A, piperidine, modified sodium alginate, corn, wheat, fructose, potassium sorbate, calcium propionate, vitamin E and modified glycerin. The insecticide components are prepared into microcapsules which wrap insecticidal active components and have a slow release effect, and the huperzine A inhibits acetylcholin esterase, increases the concentration of acetylcholine and activates a sodium ion channel; indoxacarb blocks a sodium ion channel and inhibits nerve impulse; the matrine inhibits Na < + >-ATPase and influences the membrane potential; the effects result in that nerve cells are more susceptible to indoxacarb. The modified sodium alginate changes the permeability of cell membranes and affects ion balance. Various components have a synergistic effect, so that the neurotoxicity is enhanced, the solenopsis invicta paralysis or death is finally caused, and the termite killing effect is improved. The long-acting bait combines efficient insect killing and environment friendliness, and an innovative solution is provided for prevention and control of the solenopsis invicta.

The invention provides new application of lauric acid, and researches on the inhibiting effect of lauric acid on a cardiac voltage gated sodium channel Nav1.5 and the action mode of lauric acid in electrophysiological conduction prove that natural polysaturated fatty acid lauric acid is a potential Nav1.5 sodium channel inhibitor for the first time. Electrophysiological characterization shows that lauric acid is the most effective monomer in natural polysaturated fatty acid screened for inhibiting Nav1.5, and the IC50 value is 27.40 + / -12.78 mu M.

The invention discloses a method for rapidly detecting sodium ion channel L1014F mutation of liriomyza trifoliata and a special kit, and belongs to the technical field of agricultural biology. The method comprises the following steps: extracting the DNA of the liriomyza trifoliate; carrying out PCR (Polymerase Chain Reaction) amplification by adopting two groups of primer pairs; an upstream primer of the first group of primer pair is as shown in SEQ ID NO.2, an upstream primer of the second group of primer pair is as shown in SEQ ID NO.1, and a downstream primer of the second group of primer pair is as shown in SEQ ID NO.3. Result judgment: when a 502 bp band appears in amplification of the first group of primer pairs, the L1014F site of the sample is not mutated; and when a 502 bp band appears in the amplification of the second group of primer pairs, the L1014F site of the sample is mutated. According to the method, mononucleotide variation typing can be achieved only through a conventional PCR instrument and electrophoresis, operation is easy and convenient, and the method is suitable for rapid monitoring of pyrethroid drug resistance of liriomyza trifoliate and investigation of field population resistance gene frequency.

The disclosure relates to methods of treating a neurological disorder, such as epilepsy or an epilepsy syndrome, with Compound 1 or pharmaceutically acceptable salts thereof, alone, or in combination with sodium ion (Na+) channel blockers.

The invention belongs to the field of medicinal chemistry. The invention discloses a heterocyclic compound as well as a preparation method and application thereof, and particularly relates to a series of blockers of sodium ion channels with novel structures as well as a preparation method and application thereof. The structure of the compound is shown as a general formula (I). The compounds or stereoisomers, racemes, geometric isomers, tautomers, prodrugs, hydrates, solvates or pharmaceutically acceptable salts and pharmaceutical compositions thereof can be used for treating or / and preventing sodium ion channel (Nav)-mediated related diseases.

The present invention relates to the field of pharmaceutical crystal forms, and specifically relates to crystal forms of 2-(4,4-difluoroazepin-1-yl)-N-(2-sulfamoylpyridin-4-yl)quinoline-3-carboxamide and a salt thereof, a pharmaceutical composition, and a use. The crystal forms of a compound of formula (I) and a salt thereof which are obtained in the present invention have excellent physical stability and chemical stability, and compared with free base crystal form K1 of the compound of formula (I), have significantly improved solubility, hygroscopicity and bioavailability, and are more conducive to clinical applications. Also disclosed in the present invention is a use of the crystal forms of the compound of formula (I) and the salt thereof as sodium ion channel Nav1.8 inhibitors for treating a wide range of pain.

Disclosed in the present invention are a polysubstituted pyrrolidine derivative as shown in general formula (I), a stereoisomer, a tautomer, a deuterated derivative or a pharmaceutically acceptable salt thereof; a method for preparing the compound and the use of the compound; a pharmaceutical composition comprising the compound, the stereoisomer, the tautomer, the deuterated derivative or the pharmaceutically acceptable salt thereof; the use of the compound as an inhibitor of the sodium ion channel subtype Nav1.8; and the pharmaceutical use thereof in the treatment and prevention of pain-related diseases.

The present invention belongs to the field of pharmaceutical chemistry. Disclosed in the present invention are a heterocyclic compound, and a preparation method therefor and the use thereof. Specifically, the present invention relates to a series of sodium ion channel blockers having new structures, and a preparation method therefor and the use thereof. The structure thereof is as shown in the following general formula (I). These compounds or a stereoisomer, racemate, geometric isomer, tautomer, prodrug, hydrate or solvate thereof, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition thereof can be used for treating or / and preventing related diseases mediated by a sodium ion channel (Nav).

The present invention provides an application of a substance for increasing the C-terminal content of Slack protein, which relates to the field of pharmaceutical technology. The application is the application of a substance for increasing the C-terminal content of Slack protein in the preparation of a drug for treating, assisting in the treatment and / or preventing epilepsy. The drug for treating epilepsy is a combination of a Slack mutant and Na V 1.6 Interaction interface as target, Slack mutant C-terminus and voltage-gated sodium channel Na V 1.6 N and / or C-terminal interaction, the present invention found that the voltage-gated sodium channel Na V 1.6 mediates sodium influx and activates Slack, forming a channel complex. In vivo mouse and in vitro cell experiments have shown that substances that upregulate the C-terminus of the Slack protein can reduce the current amplitude of Slack mutants, reduce epilepsy susceptibility in mouse models, and have therapeutic effects on epilepsy.

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.

The invention discloses an application of a sebastites verrucosa venom protein neoVTX. The invention finds that the sebastes verrucosa venom protein neoVTX has the functions of inhibiting a voltage-gated sodium ion channel and mediating muscle paralysis, can inhibit activities of zebra fish and grass goldfish, and can be used as a macromolecular probe template for exploring the voltage-gated sodium ion channel and explaining clinical symptoms of stab wounds of sebastes verrucosa; the compound can be further used for developing a medicine for paralyzing muscles and a medicine for relieving stabbing poisoning of sebastes verrucosa.

The invention discloses a novel modified mixed sodium ferric phosphate positive electrode material and a preparation method and application thereof. Specifically, the invention relates to a mixed sodium iron phosphate material, and the mixed sodium iron phosphate and sodium chromium iron phosphate form a sodium ion battery positive electrode material with a heterostructure. In the novel modification method provided by the invention, firstly, a precursor is prepared by a hydrothermal method (namely step S1), and then the heterostructure NFPP-NFCP is formed in situ by calcining the precursor (namely step S2). According to the modification method, the purity and crystallinity of the material are greatly improved, and the sodium ion battery positive electrode material has more excellent electrochemical performance, namely, the conductivity of the material is greatly improved, and a sodium ion channel is optimized.

The invention discloses a compound shown in a general formula (I) or a general formula (II), a stereoisomer, a tautomer, a deuterated derivative or a pharmaceutically acceptable salt thereof, a preparation method and application of the compound, and a pharmaceutical composition containing the compound, the stereoisomer, the tautomer, the deuterated derivative or the pharmaceutically acceptable salt thereof, the compound can be used as a sodion channel subtype Nav1.8 inhibitor, and can be used as a medicine for treating and preventing pain-related diseases.

The invention relates to the field of medicine crystal forms, in particular to crystal forms of 2-(4, 4-difluoroaza-1-yl)-N-(2-sulfamoyl pyridine-4-yl) quinoline-3-formamide and salt thereof, a medicine composition and application. The obtained crystal form of the compound shown in the formula (I) and the salt thereof has excellent physical stability and chemical stability, and compared with a free alkali crystal form K1 of the compound shown in the formula (I), the crystal form of the compound shown in the formula (I) and the salt thereof has obviously improved solubility and hygroscopicity and obviously improved bioavailability, and is more beneficial to clinical application. The invention further discloses the effect of the compound shown in the formula (I) and the crystal form of the salt of the compound as an inhibitor of a sodium ion channel Nav1.8, and the compound and the salt are used for treating wide pain.

The invention provides a multiphase composite iron-based polyanion sodium ion battery positive electrode material and a preparation method thereof, a planetary ball milling reinforced phase sintering method is adopted to regulate and control an initial raw material Na / Fe feeding ratio and F element loss in a high-temperature sintering process, and a series of multiphase materials with non-stoichiometric ratios are synthesized. Wherein the material with the optimal performance is a three-phase composite material of Na7Fe7 (PO4) 6F3, Na2FePO4F and Na2Fe3 (PO4) 3, and primary particles of the material have a heterojunction structure. Excellent sodium ion channels of Na2FePO4F and Na2Fe3 (PO4) 3 in the three phases are beneficial for the Na7Fe7 (PO4) 6F3 material to release high theoretical specific capacity, and the overall actual specific capacity of the material is improved; the low-strain stable lattice structure of the Na7Fe7 (PO4) 6F3 material can slow down the Na2FePO4F lattice strain, inhibit the phase change and maintain the structural integrity of the composite material in the long cycle process, so that the material has high capacity and excellent cycle performance.

The invention discloses a method and a special kit for rapidly detecting sodium ion channel K1774N mutation of methrips vigna, and belongs to the technical field of biological detection. The method mainly comprises the following steps: 1) extracting DNA (Deoxyribose Nucleic Acid) of the cowpea 2) carrying out PCR amplification by adopting two groups of primer pairs; (3) result judgment: when a 269bp band appears in amplification of the first group of primer pairs, the detected sodion channel gene mutation site K1774N of the cowpea megthrips spp sample is not mutated; when a 269bp band appears in amplification of the second group of primer pairs, the detected sodion channel gene mutation site K1774N of the cowpea megaluthrips spp sample is mutated, and when no band appears, the detected cowpea megaluthrips spp sample is not mutated. According to the application, the mutation condition of the field cowpea megthrip K1774N mutation site can be quickly and effectively detected, and the real-time state of pyrethroid resistance of the field cowpea megthrip is effectively detected.

The invention belongs to the technical field of biomedicine, and particularly relates to analgesic polypeptide SaTX-I and application thereof. The invention provides analgesic polypeptide SaTX-I, and the amino acid sequence of the analgesic polypeptide SaTX-I is as shown in SEQ ID NO. 1. The analgesic polypeptide SaTX-I provided by the invention can act on NaV1.7 channels of related species including human beings, remarkably inhibits the current intensity of the NaV1.7 sodium ion channels, reduces the induction of an organism (human or animal) to pain to a certain extent, improves the resistance of the organism to the pain, can be used as a resource to be developed into a potential analgesic drug, and has a wide application prospect. The medicine is applied to human and other animals to relieve pains. Secondly, the analgesic polypeptide SaTX-I provided by the invention can act on a NaV1.7 sodium ion channel in a targeting manner, can be applied to research on related ion channel diseases and can be used as a potential therapeutic drug for related diseases.

The invention discloses a polysubstituted pyrrolidine derivative represented by a general formula (I), a stereoisomer, a tautomer, a deuterated derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application of the compound. The invention also relates to pharmaceutical compositions comprising these compounds, stereoisomers, tautomers, deuterated derivatives or pharmaceutically acceptable salts thereof, uses of the compounds as sodium channel subtype Nav1.8 inhibitors, and uses thereof in the treatment and prevention of pain-related diseases. # imgabs0 #

Na v 1.8 To inhibit voltage-dependent sodium ion channels and for treating Na-mediated diseases such as pain and pain-related diseases and heart diseases v 1.8 To provide compounds and pharmaceutical compositions and their use for treating intervening diseases

The present invention relates to the field of biomedicine, in particular to a compound, a preparation method therefor, and a use thereof. In particular, the present application relates to a compound represented by formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, isotope-labeled compound, or polymorph thereof, a preparation method therefor, a pharmaceutical composition comprising same, and a use thereof. The compound can be used as a sodium ion channel inhibitor and has an analgesic effect. The compound of the present application also has a plurality of excellent properties.

The invention discloses a benzenesulfonamide compound as shown in a general formula (I) and a preparation method and application thereof. The series of compounds provided by the invention can be used as lead compounds of sodium ion channel inhibitors, and are expected to be used for preparing medicines for treating arrhythmia, including premature beat, acute and recurrent atrial fibrillation, heart failure, supraventricular tachyarrhythmia (PVC), ventricular premature contraction (PVC), ventricular tachycardia (VT) or ventricular fibrillation (VF).

The invention provides application of an SPAK inhibitor ZT-1a in preparation of a medicine for treating epilepsy, the structural formula of the SPAK inhibitor ZT-1a is shown in the specification, the activity of a # imgabs0 # WNK-SPAK-KCC2 / NKCC1 signal channel is increased in the first week after embryos and newborns are born, the activity of the # imgabs0 # WNK-SPAK-KCC2 / NKCC1 signal channel is remarkably reduced from brain maturation to adult, but the channel is reactivated in the epilepsy pathology state. The phosphorylation level of the Thr1007 residue of KCC2 is increased, and the function of KCC2 is reduced, so that the epilepsy symptom is aggravated. According to the invention, the novel SPAK inhibitor ZT-1a activates a transfer function of multiple regulation and control of KCC2 and NKCC1 by inhibiting the pathway, and effectively inhibits epilepsy behaviors induced by an epileptic agent and occurrence of epilepsy-like discharge of cultured neurons. The invention provides a brand new treatment means for treating epilepsy based on a neuron cation-chloride ion transporter regulation mechanism, and changes the current anti-epilepsy drug target screening which focuses on a sodium ion channel and a GABA inhibition function, so that the application has great drug research and development value.

The invention belongs to the field of medicines, and relates to a benzenesulfonamide compound as well as a preparation method and application thereof. The invention discloses a benzenesulfonamide compound as shown in a general formula (I) and a preparation method and application thereof. The series of compounds provided by the invention can be used as lead compounds of sodium ion channel inhibitors, and are expected to be used for preparing medicines for treating arrhythmia, including premature beat, acute and recurrent atrial fibrillation, heart failure, supraventricular tachyarrhythmia (PVC), ventricular premature contraction (PVC), ventricular tachycardia (VT) or ventricular fibrillation (VF).

The application belongs to the technical field of polypeptide and medicine synthesis, and particularly relates to a cyclic peptide or salt thereof inhibiting Na V 1.8 activity and application thereof in analgesia. After a series of linear peptides composed of tryptophan, lysine and arginine are obtained, the amino acids at the head and tail are cyclized by an amide bond to obtain the cyclic peptide. The cyclic peptide or salt thereof can inhibit the current of voltage-gated sodium ion channel of mammals V 1.8, and can be developed as a Na V 1.8 inhibitor. The cyclic peptide or salt thereof can act on the Na V 1.8 receptor of mammals, and can block the transmission of pain signal for a long time. The cyclic peptide or salt thereof can enhance the resistance to pain, can be developed as a potential analgesic, and is applied to relieve pain of human and other animals, and is a Na V 1.8 ion channel related disease research and a lead drug molecule for developing a drug for treating Na V 1.8 ion channel related diseases.

The invention discloses an epilepsy brain tissue induced by a sodion channel mutant gene and application of the epilepsy brain tissue. Specifically, the epilepsy brain tissue is prepared by using a sodion channel mutant gene carrying SCN1A gene c.5768Agt; the epilepsy brain-like tissue is obtained through induction culture of the embryonic stem cells with G mutation, and the epilepsy brain-like tissue obtained through culture is used for pathogenesis, treatment and drug research and development of epilepsy diseases. Meanwhile, the invention also provides a construction method of the gene carrying the SCN1A gene c.5768Agt; the invention relates to a method for obtaining brain-like tissues through induction culture of G-mutated embryonic stem cells.

The invention provides a preparation method of a sodium ion battery positive electrode active material, which comprises the following steps: disassembling a lithium iron phosphate battery to obtain a positive electrode material, the lithium iron phosphate battery being in a fully charged state; the positive electrode material, a sodium-containing reducing agent and a phosphorus source are mixed, and the sodium-ion battery positive electrode active material is obtained through a solid-phase reaction and comprises Na4Fe3 (PO4) 2P2O7. Lithium ions in the lithium iron phosphate battery in a full charge state are separated from positive lithium iron phosphate crystal lattices, so that the influence of a lithium element on the purity of the positive active material of the prepared sodium ion battery is reduced, and meanwhile, an olivine-shaped structure of lithium iron phosphate is still reserved in the positive material; the prepared sodium ion battery positive electrode active material has an open sodium ion channel, so that the sodium ion deintercalation is facilitated, and the sodium ion battery positive electrode active material can be used in a sodium ion battery.

A method for preparing a layered oxide composite material as a sodium ion battery positive electrode, relating to a sodium ion battery positive electrode material, specifically a method for preparing a layered oxide composite material. The present invention aims to solve the current layered oxide positive electrode material P2-Na 2 / 3 Ni 1 / 3 Mn 2 / 3 The modification method of O2 has the technical problems of complicated process and high cost. The present invention obtains a layered oxide material with P2 structure by co-precipitation. During the co-precipitation process, iron element is uniformly doped into the manganese position of the material to achieve iron doping modification. On the one hand, the doping of iron ions with larger ionic radius increases the unit cell volume and broadens the sodium ion channel. On the other hand, it can also suppress the Jan-Taylor effect of manganese to a certain extent, thereby improving the electrochemical performance of the material.