38 results about "NMDA receptor" patented technology

The invention discloses a ketamine derivative and application thereof in treatment of mental diseases, and belongs to the technical field of medicines. The compound or the pharmaceutical composition thereof provided by the invention can obviously improve the expression quantity of nerve cells BDNF, promote the growth of neurite, inhibit NMDA receptor signals and treat acute and chronic depression, has improved oral bioavailability compared with ketamine, and can be used for treating mental diseases such as depression.

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 discloses an aryl group-containing amine compound, its preparation method, and use. The aryl group-containing amine compound is represented by formula (I), and has the function of regulating NMDA receptor and / or monoamine transporter and / or sigma receptor activity, and can be used to prepare a medicament for treating and / or preventing diseases associated with NMDA receptors and / or monoamine transporters and / or sigma receptors, particularly central nervous system diseases. JPEG2025538201000350.jpg4951

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.

Provided herein are compounds of Formulae (I) and (X): (I) and (X), and pharmaceutically acceptable salts, isotopic variants, and combinations thereof, pharmaceutical compositions thereof and methods of use thereof for treating and preventing conditions related to NMDA receptor modulation.

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 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 invention discloses amine compounds containing substituted phenyl groups, and a preparation method and application thereof. The substituted phenyl group-containing amine compound is represented by a formula (I), and has a function of adjusting the activity of an NMDA receptor and / or a monoamine transporter, so that the substituted phenyl group-containing amine compound can be used for preparing drugs for treating and / or preventing diseases associated with the NMDA receptor and / or the monoamine transporter, especially central nervous system diseases.

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.

This invention relates to the field of biomedicine, and particularly to novel applications of the P2Y12 receptor and its antagonists. This invention discloses the use of the P2Y12 receptor as a target in screening GABA. A The application of P2Y12 receptor antagonists, specifically NMDA receptor anesthetics, in interventional drugs. This invention also discloses the use of the P2Y12 receptor antagonist ticagrelor in the preparation of GABA. A The use of receptor-based anesthetics in interventional drugs can significantly reduce GABA levels. A The duration of loss of consciousness induced by receptor-type anesthetics. This invention also discloses the effect of knocking out the P2Y12 receptor in microglia on GABA. A Application of general anesthesia induced by the receptor anesthetic sodium pentobarbital and the NMDA receptor anesthetic ketamine.

A nanocomposite according to the present invention, comprising mesoporous silica nanoparticles (MSNs), fluorescent compounds, and NMDA receptor marker antibodies, is a theragnostic nanocomposite material which enables early diagnosis of inflammatory diseases and simultaneous treatment thereof, by having the NMDA receptor marker antibodies that bind to NMDA receptors when inflammatory macrophages are activated at an inflammatory site. The nanocomposite can be widely used for the diagnosis and treatment of inflammatory diseases and monitoring of the treatment process.

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.

The invention relates to the technical field of biomedicine, and particularly discloses a central nervous system drug therapy mechanism analysis method based on system biological analysis. According to the invention, systematic biological analysis including transcriptomics, proteomics and receptor kinetics is adopted to research a therapeutic mechanism of a central nervous system drug. The combination of the three can be used for analyzing an action path through a whole chain of'gene transcription-protein function-receptor interaction ', so that the one-sidedness of a single technology is avoided, and a theoretical support is provided for system construction of central nervous system drug mechanism research. According to the invention, oxiracetam is taken as an example for explaining that the cognitive disorder improvement effect of the medicine is closely related to NMDA receptor related pathways and receptor functions through multi-omics analysis, then receptor kinetic analysis verifies that oxiracetam can inhibit NMDA receptor current and accelerate NMDA receptor desensitization, and finally inhibits NMDA receptor functions, so that the cognitive disorder improvement effect of the medicine is improved. Therefore, cognitive impairment is improved.

The application discloses preparation and application of an NMDA receptor inhibitor based on a gimalin skeleton, relates to the technical field of medicines, and particularly relates to a preparation method of gimalin derivatives shown in general formula I and II and an effect of the derivatives as neuroprotective agents, and mainly applies to anti-cerebral ischemia.

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.

Disclosed in the present invention are a substituted phenyl-containing amine compound, and a preparation method therefor and the use thereof. The substituted phenyl-containing amine compound is as represented by formula (I), has the function of adjusting the activity of an NMDA receptor and / or a monoamine transporter, and can be used in the preparation of a drug for treating and / or preventing diseases associated with the NMDA receptor and / or monoamine transporter, particularly central nervous system diseases.

The invention provides an anti-NMDA receptor antibody and application thereof. The anti-NMDA receptor antibody disclosed by the invention is specifically combined with a GluN1 subunit, a GluN2 subunit or a GluN3 subunit in an NMDA receptor, and is expected to be used for detecting the specificity of the anti-NMDA receptor antibody or detecting or diagnosing diseases related to autoimmune encephalitis.