18 results about "Reuptake" patented technology

A method of treating and attenuating L-DOPA-induced dyskinesia, comprising administering an effective dose of at least one pharmacological agent, e.g., vilazodone, having serotonin-specific reuptake inhibition (SSRI) and serotonin receptor 1A (5-HT1AR) partial agonism activity, in conjunction with L-DOPA. Other agents, such as an L-DOPA decarboxylase inhibitor, e.g., carbidopa, or other adjunct treatments may also be provided.

The present invention provides a formylpiperidine compound, a preparation method and an application thereof. The general structural formula of the formylpiperidine compound is shown in formula (I), or its isomer, or its pharmaceutically acceptable salt, ester or prodrug. The formylpiperidine compound described in the present invention is a dual-target inhibitor of 5-HT reuptake and 5-HT 1A receptor, which can overcome the problems of low clinical efficacy, poor metabolic stability and poor safety of existing antidepressant drugs, and is a compound with a novel structure, high efficiency, stability and low toxicity and having an antidepressant effect.

The invention discloses a compound with remarkable 5-hydroxytryptamine (5-HT) reuptake inhibition activity, a preparation method of the compound and application of the compound in preparation of anti-depression drugs. And the compound is a compound Oreonudine C. The invention further discloses a preparation method of the compound. The preparation method of the Oreonudine C comprises the following steps: extracting with 95% ethanol, acidifying the extract, extracting with petroleum ether, adjusting the acid water layer to be alkaline with alkali liquor, extracting with chloroform, and performing silica gel column chromatography, C18 ODS column chromatography and preparative high performance liquid chromatography on the chloroform extraction part to obtain the Oreonudine C. The invention further discloses a preparation method of the Oreonudine C. The preparation method of the Oreonudine C comprises the following steps: extracting with 95% ethanol, acidifying the extract, extracting with petroleum ether, adjusting the acid water layer to be alkaline with alkali liquor, and obtaining the Oreonudine C. In-vitro experiments show that the compound Oreonudine C remarkably inhibits reabsorption of 5-HT (the inhibition rate is 60.4%) in mouse hippocampal neuronal cells HT22, and the inhibition rate of the compound Oreonudine C is superior to that of a positive control drug amitriptyline (the inhibition rate is 53.6%). The invention provides an important candidate compound for developing efficient and novel antidepressant drugs.

The present invention provides a piperazine derivative, as shown in formula (I) or its stereoisomers and pharmaceutically acceptable salts thereof; the piperazine derivative provided by the present invention has a strong affinity for dopamine D2, D3, and 5-HT1A, 5-HT2A receptors of 5-hydroxytryptamine, and has a medium affinity for dopamine D4 and 5-HT2C, 5-HT7 of 5-hydroxytryptamine and α1-adrenaline, histamine H1 receptors, and also has a medium affinity for 5-hydroxytryptamine reuptake sites, and has no obvious affinity for cholinergic muscarinic receptors. Functionally, it is a partial agonist of D2 and 5-HT1A receptors and an antagonist of 5-HT2A receptors, and can be used to treat or prevent diseases that require regulation of one or more of dopamine D2 receptors, 5-HT1 receptors, 5-HT2 receptors, 5-HT7 receptors, α1-adrenaline receptors, histamine H1 receptors and 5-hydroxytryptamine reuptake sites.

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.

This article provides a method for treating sleep disorders (e.g., narcolepsy) in subjects who require it by administering a composition containing a triple reuptake inhibitor to the subject.

The invention comprises a method of treatment of CNS disorders by a pharmaceutical agent exhibiting combined noradrenergic, serotonergic or dopaminergic reuptake transporter inhibitory and μ-opioid agonistic activity.

The invention provides a monoamine transmitter reuptake inhibitor as well as a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for preventing or treating dopamine DA, noradrenaline NE, 5-hydroxytryptamine 5-HT and / or sigma-1 receptor mediated related diseases.

The present invention relates to a method for intelligently constructing a list of preferred 5-hydroxytryptamine reuptake inhibitors. The method comprises the following steps: constructing a functional receptor protein of a 5-hydroxytryptamine reuptake inhibitor by a homology modeling method, screening its key protein of interference with human health based on a harmful outcome pathway method, and calculating the binding energy between it and the receptor protein. The method further calculates the comprehensive effect value as the dependent variable by using an information weighting method, screening the main features of the target as the independent variable based on a variance filtering coupled Pearson correlation coefficient method, realizing the establishment of a data set, and coupling a GRU neural network with a 1D-CNN neural network to realize the intelligent construction of a list of preferred 5-hydroxytryptamine reuptake inhibitors. The present invention aims to overcome the inability of current traditional methods to comprehensively evaluate the comprehensive selection effect of the functionality of 5-hydroxytryptamine reuptake inhibitors and interference with human health, and to realize the intelligent construction of a list of preferred 5-hydroxytryptamine reuptake inhibitors with high priority by establishing a deep learning model.

Provided herein are compositions and methods for treating, diagnosing, monitoring, and / or imaging diseases, disorders, or conditions using radiopharmaceuticals that are selective for various targets. More particularly, the compositions and methods disclosed herein reduce renal retention or potential reuptake in the kidney in which the target is expressed. Various methods of reducing renal retention of radiopharmaceuticals are disclosed.

The invention provides compositions and methods for the treatment of depression and other psychiatric disorders. In particular, the invention provides sustained- or controlled-release formulations, particularly extended or slow release formulations, which include at least one monoamine oxidase inhibitor (MAOI), as well as combination therapies that include at least one MAOI and at least one norepinephrine-reuptake-inhibitor (NRI), for use in such compositions and methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Provided herein are methods of treating atypical depression in a subject in need thereof by administering to the subject compositions comprising a triple reuptake inhibitor, having the structure of Compound (1).

The invention comprises a method for treatment of ADHD or ADHD-related disorders by a pharmaceutical agent exhibiting combined serotonergic or noradrenergic reuptake transporters and monoamine receptor activity.

The invention discloses an application of Baf-A1 in increasing the yield of mesenchymal stem cell derived extracellular vesicles. The invention reveals that Baf-A1 significantly increases the yield of iPSC-MSC-EVs through a dual mechanism of promoting secretion and inhibiting reuptake for the first time, and does not affect the therapeutic efficacy of Baf-A1. Compared with the untreated iPSC-MSC-EVs, the EVs generated by the iPSC-MSC treated by the Baf-A1 have the same protection effect on ALI and IBD under the same dosage. Therefore, the addition of the Baf-A1 in the iPSC culture process may be a potential strategy for enhancing the yield of the iPSC-MSC-EVs, thereby improving the challenge of low yield of the iPSC-MSC-EVs. In-vivo and in-vitro experiments prove that the yield of EVs can be increased by treating iPSC-MSC by using Baf-A1, and the Baf-A1 can exert the same curative effect as that of an untreated group in treatment of diseases such as acute liver injury and colitis under the condition of ensuring biological safety.

The invention discloses a compound with remarkable noradrenaline (NE) reuptake inhibition activity and application of the compound in preparation of an anti-depression drug. The compound is a compound Oreonudine F. The preparation method of the compound comprises the following steps: extracting an overground part of wild poppy by using 95% ethanol, acidifying an extract, extracting by using petroleum ether, adjusting an acid water layer to be alkaline by using alkali liquor, and extracting by using chloroform. The chloroform extraction part is subjected to silica gel column chromatography, C18 ODS column chromatography, preparative high performance liquid chromatography separation and the like, and the compound Oreonudine F is obtained. In-vitro activity test results show that the compound Oreonudine F significantly inhibits reabsorption of NE (the inhibition rate is 45.6%) in mouse hippocampal neuronal cells HT22, and the inhibition rate of the compound Oreonudine F is superior to that of a positive control drug amitriptyline (the inhibition rate is 35.5%). The invention provides an important candidate compound for developing efficient and novel antidepressant drugs.

Provided herein is a method of treating atypical depression in a subject in need thereof by administering to the subject a composition comprising a triple reuptake inhibitor having the structure of Compound (1). TIFF2025508878000026.tif25128