Method for detecting metabolic performance of new chemical entity in different species of liver microsomes

Abstract

The invention discloses a method for detecting the metabolic performance of a new chemical entity in different species of liver microsomes, which comprises the following steps: in a reaction system containing a buffer solution, liver microsomes, a substrate, MgCl2 and NADPH, screening out an optimal reaction condition by taking the metabolic rate of the substrate as a reference to obtain a human liver microsome incubation system. According to the establishment method of the human liver microsome incubation system, rat, mouse, dog and monkey liver microsome incubation systems are sequentially established. The method comprises the following steps: performing in-vitro metabolism test on a new chemical entity in incubation systems of different species of liver microsomes, performing positive group reaction by using a substrate, and setting a negative group without adding NADPH and a blank group without adding liver microsomes; and identifying a metabolism result after testing. According to the method for detecting the metabolic performance of the new chemical entity in different species of liver microsomes, false positive and false negative results can be avoided, the reliability of an identification result is improved, and a reliable basis is provided for promoting research and development of new drugs.

Description

technical field [0001] The invention relates to a method for detecting the metabolic properties of new chemical entities in different species of liver microsomes. Background technique [0002] During the research and development of new chemical entities, it is necessary to study their metabolic properties. By obtaining and evaluating relevant metabolic information, the success rate of new drug screening can be effectively improved and development costs can be reduced. In the prior art, the detection method for the metabolic performance of new chemical entities in different species of liver microsomes has low accuracy and is likely to cause false positive or false negative results. When false positive or false negative results are generated, it is impossible to quickly identify and judge the cause of false positive or false negative results, which brings a lot of inconvenience to the development of new drugs. In the prior art, there is a lack of verification tests for the de...

AI Technical Summary

Problems solved by technology

In the prior art, the detection method for the metabolic performance of new chemical entities in different species of liver microsomes has low accuracy and is likely to cause false positive or false negative results

When false positive or false negative results are generated, it is impossible to quickly identify and judge the cause of false positive or