7 results about "AMPA receptor activity" patented technology

The application belongs to the technical field of biological medicine, and discloses a synthesis method of aryl F-18 labeled sulfuryl chloride and application of the aryl F-18 labeled sulfuryl chloride in amine compound labeling. The method takes thiophenol derivative as a labeling precursor, obtains F-18 labeled thiophenol intermediate through photocatalytic aryl F-18 fluorination reaction, and then obtains aryl F-18 labeled sulfuryl chloride through N-chlorosuccinimide oxidation chlorination. The obtained aryl F-18 labeled sulfuryl chloride (4-[ 18 F] fluorobenzenesulfonyl chloride) can occur sulfurylization reaction with various amine compounds at room temperature, and the radiochemical conversion rate is as high as 98%. The application is successfully applied to novel synthesis of AMPA receptor PET imaging agent[ 18 F]2 (the conversion rate is 96%, which is much higher than 13% reported in the literature). The application has the advantages of mild reaction condition, high conversion rate and wide substrate application range, and provides an efficient method for innovative preparation of F-18 labeled PET probes.

To provide a method and a computing device that allow for more effective determination regarding which patients will experience drug efficacy, and which patients will experience adverse drug events, and that provide personalized recommendations for patients regarding dose, the frequency of drug administration, and drug choice.SOLUTION: A method for identifying patients diagnosed with treatment resistant or refractory depression, pain or other clinical indications, who are eligible to receive N-methyl-D-aspartate receptor antagonist, glycine receptor beta modulator, or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor-based therapies.SELECTED DRAWING: None

This invention relates to the use of (i) a 5-HT2A agonist (including 5-HT2A agonists that bind to a BDNF receptor, e.g., a 5-HT2A agonist that binds to the TrkB receptor or p75NTR), (ii) a therapeutic agent that promotes neuroplasticity by stimulation of the 5-HT2A receptor, (iii) a therapeutic agent that releases BDNF by stimulation of the 5-HT2A receptor (including those therapeutic agents that stimulate the 5-HT2A receptor and bind to a TrkB receptor or p75NTR), (iv) an AMPA positive allosteric modulator, (v) a therapeutic agent that promotes neuroplasticity by stimulation of the AMPA receptor, (vi) a therapeutic agent that releases BDNF by stimulation of the AMPA receptor, or (vii) an NMDA receptor positive allosteric modulator (such as a stinel compound) in the treatment of a psychiatric condition in which depressive symptoms are prominent, including major depressive disorder (MDD), bipolar disorder, post-traumatic stress disorder, substance use disorder, and depression-related aspects of schizophrenia (e.g. negative symptoms) in select patients who, for instance, have objectively determined cognitive impairment or poor cognition (such as objectively determined impaired learning and / or memory) and / or certain EEG characteristics.

The invention belongs to the technical field of biological medicine, and particularly relates to an anti-depression drug, a composite microsphere and a preparation method of the composite microsphere, and the anti-depression drug provided by the invention has excellent inhibitory activity on 5-HT reuptake and AMPA receptors and has an excellent treatment effect. In addition, the anti-depression drug microspheres provided by the invention are high in encapsulation efficiency, large in drug loading capacity, excellent in drug sustained release effect, better in human body absorption effect, capable of remarkably reducing the drug use frequency and / or the use dosage and small in toxic and side effects.

The present application provides compounds of Formula (I) and related compositions and methods, including methods of therapy for treating nervous system diseases and disorders, including multiple sclerosis (MS) and amyotrophic lateral sclerosis (ALS), and methods for in vivo imaging of AMPA receptors or surrogates thereof in the brain. (I)

The invention belongs to the technical field of biological medicine, and discloses a synthesis method of aryl F-18 labeled sulfonyl chloride and application of the aryl F-18 labeled sulfonyl chloride in amine compound labeling, the method comprises the following steps: by taking a thiophenol derivative as a labeling precursor, obtaining an F-18 labeled thiophenol intermediate through photocatalytic aryl F-18 fluorination reaction; and then carrying out oxidative chlorination by using N-chlorosuccinimide to obtain aryl F-18 labeled sulfonyl chloride. The obtained aryl F-18 labeled sulfonyl chloride (4-[18F] fluorobenzene sulfonyl chloride) can be subjected to sulfonylation reaction with various amine compounds at room temperature, and the radiochemical conversion rate is as high as 98%; the method is successfully applied to novel synthesis of the AMPA receptor PET developer [18F] 2 (the conversion rate is 96% and is far higher than 13% reported in literature). The method is mild in reaction condition, high in conversion rate and wide in substrate application range, and an efficient method is provided for innovative preparation of the F-18 labeled PET probe.