21 results about "NMDA receptor" patented technology

Disclosed in the present invention are an aryl-containing amine compound, a preparation method therefor and a use thereof. The aryl-containing amine compound is represented by formula (I), and has the function of regulating the activity of an NMDA receptor and / or a monoamine transporter and / or a sigma receptor. Thus, the compound can be used for preparing drugs for treating and / or preventing diseases associated with an NMDA receptor and / or a monoamine transporter and / or a sigma receptor, especially central nervous system diseases.

The present application relates to endogenous NMDA receptor subtypes in brain tissue and their assembly and structure. The present application provides a method for evaluating the function of endogenous NMDA receptors in brain tissue (cortex and hippocampus), comprising obtaining data on the structure and / or quantity of endogenous NMDA receptors (NMDAR) in the brain tissue, wherein the NMDA receptor comprises a GluN1-N2A-N2B triheteromer; and comparing the structure and / or quantity of the GluN1-N2A-N2B triheteromer with a reference structure and / or quantity reference value, thereby giving an evaluation result of the function of endogenous NMDA receptors in brain tissue. The present application also provides a device for performing the evaluation and a method for drug screening based on changes in the structure and / or quantity of specific NMDA receptors.

The invention belongs to the technical field of biological medicine, and relates to a recombinant NMDA receptor antibody and application thereof. The invention relates to a recombinant NMDA receptor antibody Tat-DiN2B and application of the recombinant NMDA receptor antibody Tat-DiN2B in preparation of a medicine for inhibiting neurological function defect. The nerve injury which can be inhibited by the Tat-DiN2B comprises cortical neuron excitatory toxicity injury, acute hippocampal brain slice excitatory toxicity injury and cerebral ischemia injury. Meanwhile, the Tat-DiN2B can also be used for improving the dyskinesia and anxiety level after cerebral ischemia. The Tat-DiN2B disclosed by the invention is constructed by taking a gene synthesized by Tat and DiN2B as a template through the steps of PCR (Polymerase Chain Reaction) amplification, enzyme digestion, transformation, transfection, expression, purification and the like, and a DNA (Deoxyribonucleic Acid) sequence of the Tat-DiN2B is as shown in SEQ ID No.1.

The present invention belongs to the field of pharmaceuticals. Disclosed in the present invention are a class of salt compounds of isosorbide mononitrate derivatives and the use thereof. Salts formed by the isosorbide mononitrate derivatives of the present invention and D-cycloserine exhibit dual activities as a nitric oxide donor and a partial NMDA receptor agonist. The present invention further relates to the use of the salts formed by the isosorbide mononitrate derivatives and D-cycloserine in a drug for treating cerebral stroke or the recovery period of cerebral stroke.

The invention provides application of a compound shown in a formula (III) or pharmaceutically acceptable salt thereof in preparation of a medicine for treating and / or preventing diseases related to an NMDA receptor. The compound has good antagonistic activity on the NMDA receptor (especially a GluN1 / GluN3A receptor).

The present invention relates to a NMDA receptor antagonist and a use thereof. The NMDA receptor antagonist of the present invention is a compound of formulas II and III below, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a tautomer, a solvate, an isotopic substituent, a polymorphic substance, a prodrug or a metabolite thereof. The present invention also provides a pharmaceutical composition comprising these compounds, and a use of these compounds in treating or preventing NMDA receptor-mediated diseases.

The present invention relates to a support coated with eukaryotic cells overexpressing a polypeptide comprising a human NMDA receptor or a variant thereof for use in a microscopic immunofluorescence assay; a support comprising said cells and mock transfected cells, wherein said cells and said mock transfected cells are spatially separated; a kit comprising said cells or said support, and the use of said cells or said support or a polypeptide comprising a human NMDA receptor or a variant thereof for producing a signal free of artefacts for detecting autoantibodies directed against a human NMDA receptor.

The invention relates to the technical field of environmental endocrine disruptors, and discloses a biomarker for detecting EDC-induced glutamic acid synaptic dysfunction and a detection method thereof. The biomarker combination comprises molecules selected from at least one group of the following: presynaptic end function related proteins: plasma or cerebrospinal fluid (CSF) exosome levels including but not limited to synapsin-1 and vesicular glutamate transporter 1 (VGLUT1); proteins related to post-synaptic density and NMDA receptor functions include, but are not limited to, post-synaptic density protein 95 (PSD95), the phosphorylation level of a GluN1 subunit or soluble fragments thereof in CSF; the invention relates to astrocyte-neuron coupling related molecules. According to the invention, a multi-dimensional biomarker combination containing a presynaptic terminal function, a post-synaptic density and receptor function, astrocyte-neuron coupling and endoplasmic reticulum stress and calcium homeostasis is constructed, so that systemic evaluation of EDC-induced glutamic acid synaptic dysfunction is realized.

The present invention relates to compounds inhibiting the toxic activity of extrasynaptic NMDA receptors, in particular by inhibiting the formation of NMDA receptor / TRPM4 complexes. In particular, the present invention relates to diamine-based compounds according to general formula I and their use in medicine, in particular for treating neurological diseases such as neurodegenerative diseases.

The present application relates to the field of biological medicine, and particularly relates to a new use of CSF1R and an inhibitor thereof, and discloses application of CSF1R as a target point in screening GABA A receptor, NMDA receptor, beta 2A receptor anesthetics intervention drugs. The present application also discloses application of a CSF1R inhibitor, PLX5622, in preparing GABA A , NMDA, beta 2A receptor anesthetics intervention drugs; and the present application can significantly shorten the duration of GABA A , NMDA, beta 2A receptor anesthetics induced loss of consciousness.

The invention provides application of esketamine in preparation of hyperalgesia drugs, and relates to the technical field of clinical medicine. Clinical tests and animal experiments are combined, it is systematically proved that sub-anesthetic dose esketamine can effectively relieve diabetic hyperalgesia, and a novel molecular action mechanism of esketamine is disclosed. Preliminary tests and animal experiments show that the scheme can significantly improve the mechanical pain threshold and reduce the pain score, and the effect is exact. In mechanism, it is clarified for the first time that esketamine regulates and controls downstream PI3K / Akt / GSK-3beta signal channels by inhibiting excessive activation of an NMDA receptor, and abnormal expression and membrane transport of a GLuR1 receptor are reduced, so that central sensitization is reversed. The scheme has the advantages of quick response, no opioid drug dependence, clear mechanism and the like, provides a new safe, effective and clear-target analgesic strategy for clinical treatment of diabetes-related neuropathic pain, and has good transformation and application prospects.

Described herein are pharmaceutical compositions comprising Compound I, and pharmaceutically acceptable salts thereof, and methods of use thereof for treating conditions associated with NMDA receptor modulation.

Provided herein are modified forms of Conantokin peptides, including, modified Con-P peptides, nucleic acids encoding the same and compositions thereof. Further provided are nucleic acid molecules encoding for chimeric modified conantokin polypeptides to be expressed in or on a membrane of a target cells, compositions comprising the same and uses thereof for treating various neurodegenerative conditions.

Provided is a pharmaceutical composition including a metal channel activator and an NMDA receptor antagonist. Also provided is a method of treating a depressive disorder, including administering the pharmaceutical composition. Also provided is a method of treating a neurological or neurodegenerative disorder, including administering the pharmaceutical composition. Also provided is a method of treating a pain disorder, including administering the pharmaceutical composition.

The present invention relates to a support coated with eukaryotic cells overexpressing a polypeptide comprising a human NMDA receptor or a variant thereof for use in a microscopic immunofluorescence assay; a support comprising said cells and mock transfected cells, wherein said cells and said mock transfected cells are spatially separated; a kit comprising said cells or said support, and the use of said cells or said support or a polypeptide comprising a human NMDA receptor or a variant thereof for producing a signal free of artefacts for detecting autoantibodies directed against a human NMDA receptor.

The present invention discloses a neurosynaptic structure for a spiking neural network, wherein the neurosynaptic structure comprises: one or more input ports, one or more synaptic elements, each synaptic element connected to at least one of the input ports and configured to receive an input signal and to output a weighted postsynaptic signal. Furthermore, the neurosynaptic structure comprises a neuron connected to the one or more synaptic elements. The neurosynaptic structure is provided with different feedback and control structures such as AMPA-, GABA-, and NMDA receptors, axon-, dendrite- and neuron back-propagation channels and / or an astrocytes structure.

The application relates to the technical field of biotechnology, and particularly discloses a recombinant NMDA receptor protein and application thereof, wherein the recombinant NMDA receptor protein comprises an amino acid sequence shown in SEQ ID No. 1. The application further provides a cell stably overexpressing the recombinant NMDA receptor protein and applying the cell to preparation of an anti-NMDA receptor antibody encephalitis detection product. The recombinant NMDA receptor protein is constructed by combining a core sequence of HSP70 protein with a complete sequence of the NMDA receptor protein, so that the expression amount of the recombinant NMDA receptor protein is higher, and the binding capacity with the anti-NMDA receptor antibody is stronger. The cell stably overexpressing the recombinant NMDA receptor has a higher binding efficiency with the anti-NMDA receptor antibody, the sensitivity of a detection reaction is further improved, and the detection result is more accurate.

The present invention relates to compounds inhibiting the toxic activity of extrasynaptic NMDA receptors, in particular by inhibiting the formation of NMDA receptor / TRPM4 complexes. In particular, the present invention relates to diamine-based compounds according to general formula I and their use in medicine, in particular for treating neurological diseases such as neurodegenerative diseases.

An application of GluN2A and an NMDA receptor containing GluN2A as targets in screening antidepressant drugs, which may achieve rapid and low-cost screening of antidepressant drugs. Specifically, provided is a use of GluN2A, a binding fragment thereof or an NMDA receptor containing GluN2A in screening antidepressant drugs or in the preparation of a reagent for screening antidepressant drugs. Also provided are a method and apparatus for screening antidepressant drugs, and a kit.