65 results about "NMDA receptor" patented technology

The present invention relates to compounds that inhibit the toxic activity of the extrasynaptic NMDA receptor, in particular by inhibiting the formation of the NMDA receptor / TRPM4 complex. In particular, the present invention relates to diamino compounds according to general formula I and their use in medicine, in particular for the treatment of nervous system diseases, such as neurodegenerative diseases.

The present disclosure relates to compositions, kits, and methods of treating CNS diseases and disorders using a combination of a muscarinic receptor positive modulator and an NMDA receptor positive allosteric modulator.

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.

The invention discloses application of a cannabidiol analogue CIAC001 in preparation of a medicine for treating Alzheimer's disease, and relates to the technical field of medicine. The application comprises the following steps: step 1, medicine extraction: extracting CIAC001, an NMDA receptor antagonist and a cholinesterase inhibitor according to a ratio of 1: 5: 5 into a medicine carrying needle cylinder; 2, medicine heating, wherein a heating assembly is started to conduct pulse heating on the medicine in the medicine carrying needle cylinder; 3, nursing the patient: heating and nursing the injection part of the patient by using a nursing assembly; 4, medicine injection: pushing a pushing head, puncturing a needle into the injection part of the patient, and injecting the medicine into the body of the patient; and 5, observing and treating side reactions: taking down the injection device after the drug reaction is complete, observing the side reaction condition of the patient, and starting a temperature regulator to cool the patient. The medicine activity can be effectively improved, side effects of the medicine on patients are reduced, and therefore the treatment effect of the medicine is enhanced.

Provided herein are methods for improving working memory and / or executive function in a subject suffering from Huntington's Disease, comprising administering to the subject SAGE-718, an investigational positive allosteric modulator of the NMDA receptor.

The present disclosure relates to the subcutaneous administration of compound (I) or a pharmaceutically acceptable salt thereof for treating diseases or disorders mediated by negative allosteric modulation or inhibition of NR2B-containing NMDA receptors, including but not limited to depressive disorders (e.g., major depressive disorder, treatment-resistant depression, suicidal tendency in major depressive disorder, major depressive disorder with suicidal ideation, major depressive disorder with suicidal ideation and intent, suicidal tendency, and seasonal affective disorder). The present disclosure also relates to the use of compound (I) or a pharmaceutically acceptable salt thereof in the treatment of treatment-resistant depression in patients with major depressive disorder. 【Chemical 1】 TIFF2025518778000031.tif20170

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 invention provides application of a compound shown in a formula (I) 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 inhibitory activity on the NMDA receptor (especially a GluN1 / GluN3A receptor).

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.

Compounds are provided for modulating NMDARs generally, or for treating a NMDARé-dependent condition more specifically, by contacting the NMDA receptor or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): (I) or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein Ra, R1, R2, R3, R4, and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

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

To provide improved NMDAR protein constructs for detection of NMDAR autoantibodies and for treatment of autoimmune diseases associated with NMDAR autoantibodies.SOLUTION: Provided is a soluble N-methyl-D-aspartate receptor (NMDAR) protein construct comprising one or more NMDAR autoantibody epitopes, the construct comprising an extracellular domain (ECD) of the NMDAR subunit GluN1 or a fragment thereof and an ECD of at least one of the NMDAR subunits GluN2A, GluN2B, GluN2C or GluN2D, or fragment thereof.SELECTED DRAWING: None

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 compounds of formula (I):for use as peripheral NMDA receptor antagonists.

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.

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

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 compounds that inhibit the toxic activity of extrasynaptic NMDA receptors, particularly by inhibiting the formation of the NMDA receptor / TRPM4 complex. In particular, the present invention relates to diamine compounds according to general formula I and their use in medicine, especially in the treatment of neurological disorders such as neurodegenerative disorders.

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 a nerve synapse structure for a spiking neural network, and the nerve synapse structure comprises one or more input ports; and one or more synaptic elements, each synaptic element connected to at least one input port and configured to receive an input signal and output a weighted post-synaptic signal. In addition, the neurosynaptic structure includes neurons connected to the one or more synaptic elements. The neurosynaptic structures are provided with different feedback and control structures, such as AMPA, GABA and NMDA receptors, axon, dendritic and neuronal back propagation channels, and / or astrocyte structures.

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.

The present invention relates to NMDA receptor antagonists and uses thereof. The NMDA receptor antagonist disclosed by the invention is a compound shown as a formula I, and pharmaceutically acceptable salt, enantiomer, diastereoisomer, tautomer, solvate, isotope substitute, polymorphic substance, prodrug or metabolite thereof. The invention also provides pharmaceutical compositions containing the compounds, and applications of the compounds in preparation of drugs for treating or preventing NMDA receptor mediated diseases. # imgabs0 #

The present disclosure relates to subcutaneous doses of Compound (I), or a pharmaceutically acceptable salt thereof, for the treatment of diseases or disorders mediated by negative allosteric modulation or inhibition of NMDA receptors containing NR2B, including, but not limited to, depressive disorders, such as, for example, neurological disorders. Comprising major depressive disorder, treatment of resistant depression, suicide tendency in major depressive disorder, major depressive disorder with suicide thought, major depressive disorder with suicide thought and suicide intention, suicide tendency and seasonal affective disorder. The disclosure also relates to the use of Compound (I) or a pharmaceutically acceptable salt thereof in the treatment of resistant depression in the treatment of patients suffering from severe depressive disorder. Formula (I) imgabs0 #