65 results about "Ion channel blocker" patented technology

The invention pertains generally to the field of drug discovery science. More specifically, the invention refers to a drug screening assay and device that is used to test the effect of specific chemical compounds as use dependent ion channel blockers. The invention includes a unique method for stimulating cells with photoconductive stimulation and reading consequent cell ion channel activity with the optical imaging of fluorescent dyes.

The invention provides compounds, compositions, methods, and kits for the treatment of pain, itch, and neurogenic inflammation.

The present invention describes a novel treatment for movement disorders, including tardive dyskinesia, tic disorders, Tourette's syndrome, and blepharospasm, and other focal dystonias. The treatment of the present invention utilizes agents that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of a single agent, for example acamprosate. Alternatively, separate agents having these activities can be combined and administered together. The invention also provides a third agent that acts as a non-competitive NMDA-receptor blocking agent or ion channel blocker that augments the effect of the primary treatment. A particularly preferred ion channel blocking agent is magnesium. Alternatively, magnesium can be administered alone for prevention and treatment of movement disorders.

The invention discloses application of bulleyaconitine A (BLA) used as a state-independent sodium ion channel blocker to the analgesia, and relates to application of a medicine, in particular to application of aconitine alkaloids to the analgesia. The application of the bulleyaconitine A used as the state-independent sodium ion channel blocker to the analgesia is characterized in that the BLA only blocks a neuron sodium ion channel in an open state in a state dependence way, and does not interact with a neuron sodium ion channel in a resting state or an inactivation state. Compared with other analgesic medicines, the medicine in which the bulleyaconitine A is taken as an active ingredient has the advantage that the analgesic side effect is relatively small.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

Disclosed herein are an N-(pyrazolylmethyl)arylsulfonamide derivative useful as a calcium ion channel blocker, a pharmaceutically acceptable salt thereof, and the medicinal use thereof as a therapeutic agent using its calcium ion channel blocking effect.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.

The invention relates to the application field for treating medicament resistance of antibiotic series medicaments for human body or biology of sodium ion channel regulating agent series compounds and medical salts and esters, especially relates to new application for treating medicament resistance of antibiotic series medicaments for human body or biology of the compounds, According to the sodium ion channel regulating agent series compounds and medical salts and esters of the invention, the medicament resistance for human body or biology generated by the antibiotic series medicaments can beeffectively treated, thereby improving the sensitivity rate and the potency of the antibiotic series medicaments for various viruses.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

The invention provides a fluorescent cell model for screening an M2 ion channel blocker for influenza virus, and the cell model is a cell containing pH sensitive fluorescent materials. Meanwhile, the invention also provides a method for screening the M2 ion channel blocker for the influenza virus by the cell model, which is to detect the change of fluorescent values in the cell model under the condition of an acidic buffer. The invention has the advantages that the H+ flowing condition through the M2 ion channel is directly reflected by detecting the change of the fluorescent values reflecting pH in the cell; and the M2 ion channel blocker screening method established by the cell model has definite mechanism of drug action, is simple and convenient, quick and direct, and is suitable for high-flux accurate screening of the M2 ion channel blocker.

The presently described subject matter relates to isolated spider venom peptides, which are used as potent and selective ion channel blockers, and to a composition and methods for treatment of pain.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

The present invention relates to a method of designing an ion channel blocker for an ion channel which includes providing an ion channel having an external vestibule portion and raising an antibody, binding portion, probe, or ligand specific to the external vestibule portion of the ion channel, where the antibody, binding portion, probe, or ligand inhibits ion transport through the ion channel. The present invention further relates to a method of inhibiting ion transport through an ion channel, a method for screening a drug for effectiveness as an ion channel blocker, and an antibody, binding portion, probe, or ligand.

Described herein are methods of preserving a tissue of a subject, such as a brain or a portion thereof. The methods include washing the tissue by perfusing the tissue with a wash fluid comprising an aqueous solution; fixing the tissue by perfusing the tissue with a fixation fluid comprising an aldehyde; and cryoprotecting the tissue by perfusing the tissue with a cryoprotection fluid comprising a vitrification agent. The wash fluid, the fixation fluid, and / or the cryoprotection fluid can include a dye or a contrast agent to monitor perfusion of the fluid through the tissue. In certain embodiments, the cryoprotection fluid has a vitrification temperature of about −80° C. or higher. The wash fluid can further include one or more of an ion channel blocker, a calcium chelator, a thrombolytic agent, an anti-platelet, a respiratory poison, or a synaptic poison. Also described herein are methods of analyzing the preserved tissue.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.

The invention discloses a 1,2-diketone naphthalene compound which has a general structural formula (I) described in the specification, wherein Ar represents benzene ring, naphthalene ring, quinoline ring or isoquinoline ring, naphthalene diimide ring or coumarin ring; amino acid is directly connected with the Ar; when a substituent group exists on the Ar, R is an electron-withdrawing, electron-donating or neutral group. The invention further discloses a preparation method of the compound and application of the compound to preparation of inflammation-resistant and immunocompetence-resistant drugs. The compound is relatively good in inflammation and immunological competence resistance, is a CRAC (Ca<2+> release activated Ca<2+>) blocker with a novel structure, and can be used as a lead compound of the inflammation-resistant and immunocompetence-resistant drugs. According to the preparation method, the reaction condition is mild, raw materials are cheap and easily available, and the operation and the post-treatment process are simple.

The present invention relates to the use of blockers of ion channels regulated by the SUR subunit, for the treatment and / or prevention of eye diseases associated with ischemia and / or retinal excitotoxicity.

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.

The invention relates to novel application of sodium ion channel blocker compounds, derivatives thereof as well as pharmaceutical salts and esters of the sodium ion channel blocker compounds and the derivatives thereof in the application field of improving the sleeping quality of people and organisms, in particular to novel application that the compounds can both remarkably improve the sleeping quality of the people and the organisms when used singly and jointly used with sleeping and sedative drugs. A sodium ion channel blocker of the invention is mainly: 1, amino perhydrogenated quinazoline compounds as well as pharmaceutically salts and esters thereof; and 2, diguanidino hydrogenated purine ring compounds as well as pharmaceutically salts and esters thereof.

The invention relates to a medicine composition for treating age-related hearing loss (ARHL). The medicine composition is characterized by comprising calcium ion channel blockers and / or free radical scavengers in effective treatment dosage. According to the medicine composition, two kinds of medicine with approvals of food and drug administration (FDA), i.e. the calcium ion channel blockers and free radical scavengers (antioxidant) relevant to free radical metabolic pathways are used, the two kinds of different chemical medicines are combined to be used in a synergistic action mode, the ARHL treatment effect can be improved, and in addition, the toxic and side effect of the medicine is reduced. The innovation points of the medicine composition are mainly in the following two aspects: (1) the medicine composition is focused on 11000 kinds of medicine with FDA approvals, and the medicine has high pharmacological activity and low side effects; and (2) medicine selected in the medicine composition respectively acts on different cell-molecle mechanism target sites, and the synergistic effect can be generated after the two kinds of medicine are combined to be used.