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A compound having inhibitory activity against the glycine transporter

A technology for inhibiting activity and compounds, which is applied in the direction of drug combinations, chemical instruments and methods, and cyclic peptide components, and can solve problems such as the same structure of compounds

Active Publication Date: 2015-08-19
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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  • A compound having inhibitory activity against the glycine transporter
  • A compound having inhibitory activity against the glycine transporter
  • A compound having inhibitory activity against the glycine transporter

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% NZ CASE, 0.2% yeast extract and 0.2% calcium carbonate to 7.0, at 120°C Sterilize under moist heat for 20 minutes. Then inoculate an appropriate amount of strain CGMCC No.0792 under aseptic operation, shake culture at 28° C. and 180 rpm for 3 days, and use it as a seed culture solution.

[0035] Then add 1% glycerol, 0.5% glucose, 1% soluble starch, 0.1% (NH 4 ) 2 SO 4 ,

[0036] 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 f...

Embodiment 2

[0040] Example 2 Inhibitory Experiment on Rat Neuroglial Cells

[0041] 1. Specimen

[0042] 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.

[0043] 2. Experimental cells

[0044] 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 compounds produced by microorganisms having inhibitory activity against the glycine transporter in mammalian glial cells. Background technique [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 similar ...

Claims

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Application Information

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Patent Type & Authority Patents(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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