New compound with inhibiting activity to glycine transporters

A technology for inhibiting activity and compounds, which can be used in drug combinations, chemical instruments and methods, cyclic peptide components, etc., and can solve problems such as the same structure of compounds

Active Publication Date: 2013-10-30
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The compound of the present invention is based on the research of the Chinese patent application CN1535980A, and is obtained by using exogenous amino acid incorporation fermentation technology. So far, no compound with the same structure as the compound of the present invention and significant inhibitory activity on glycine transporters has been found.

Method used

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  • New compound with inhibiting activity to glycine transporters
  • New compound with inhibiting activity to glycine transporters
  • New compound with inhibiting activity to glycine transporters

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation of embodiment 1 compound C6035G

[0034] 1. Adjust the pH of the liquid medium containing 1% glucose, 2.5% soluble starch, 0.3% cottonseed meal, 0.5% fish meal, 0.3% NZCASE, 0.2% yeast extract and 0.2% calcium carbonate to 7.0 at 120°C Sterilize with moist heat for 20 minutes. Then, an appropriate amount of strain CGMCC No.0792 was inoculated under aseptic operation, shaken at 28° C. and 180 rpm for 3 days, and used as a seed culture solution.

[0035] Then add 1% glycerol, 0.5% glucose, 1% soluble starch, 0.1% (NH 4 ) 2 SO 4 , 0.05% MgSO 4 ·7H 2 O, 0.2% calcium carbonate and L-isoleucine 0.2% liquid culture medium 100ml adjust pH to 7.0 and pack in the 500ml Erlenmeyer shaker flask, prepare 100 bottles altogether, in 120 ℃, moist heat sterilization 20 minutes. Then, under aseptic operation, the above-mentioned seed culture solution was added thereto according to 10% inoculum amount, and cultured with shaking at 28° C. and 180 rpm for 6 days.

[0...

Embodiment 2

[0039] Example 2 Inhibitory Experiment on Rat Neuroglial Cells

[0040] 1. Specimen

[0041]Compound C6035G was dissolved in dimethyl sulfoxide and prepared to a concentration of 10 mg / ml, diluted with sterilized water to the target concentration for use.

[0042] 2. Experimental cells

[0043] Rat glial cells C6.

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Abstract

The invention discloses a new compound with inhibiting the activity to glycine transporters, which is shown in a formula (I). The compound can be used for treating mental disorders associated with NMDA glycine receptors. The invention also discloses a preparation method of the compound shown in the formula (I), a pharmaceutical composition taking the compound as an active ingredient, and the application of the compound in preparation of drugs for treating mental disorders reacting with NMDA glycine receptors.

Description

technical field [0001] The present invention relates to novel compounds produced by microorganisms having inhibitory activity against the glycine transporter in mammalian glial cells. technical background [0002] The current academically recognized physiological cause of schizophrenia is caused by the decrease of glutamate nerve signal transduction function dependent on N-methyl-D-aspartic acid (NMDA) in the brain. Among them, the NMDA receptor contains glycine and polyamine binding sites, which can activate NMDA receptors by combining with glycine, so as to treat schizophrenia and other mental diseases related to NMDA receptor dysfunction. [0003] In recent years, a large number of molecular biology studies have found that there are two types of NMDA glycine receptors, GlyT-1 and GlyT-2, and GlyT-1 is further divided into three types: GlyT-1a, GlyT-1b and GlyT-1c. These NMDA receptors can be blocked by some inhibitors or antagonists, thereby inducing negative symptoms si...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/12A61K38/12A61P25/18C12P21/04
Inventor 褚以文王辂赵子翰叶丽娟
Owner CHENGDU UNIV
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