Cell line and method for detecting biological activity of dopamine D4 target compound
A technology of biological activity and detection method, which is applied in the field of detection of biological activity of dopamine D4 target compounds and cell lines for detection of biological activity of dopamine D4 target compounds, can solve the problems of lack of methods for detection of biological activity, and achieve High accuracy, high signal window and good repeatability
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Embodiment 1
[0097] Example 1 is designed as a functional validation of HEK293 / D4 cells.
[0098] 1.1 Purpose of the experiment
[0099] HEK293 / D4 cells were constructed and their activated cAMP responses were verified.
[0100] 1.2 Experimental steps
[0101] 1. Construction of HEK293 / D4 cells
[0102] (1) Digest HEK293 cells with trypsin and plate them into 6-well plates, 1x10 per well 5 cells at 37°C, 5% CO 2 grow overnight in a cell culture incubator;
[0103] (2) Take out a tube of D4 receptor lentivirus from liquid nitrogen, put it on ice to thaw, and spin it at 1000rpm after thawing to make the solution adhering to the tube wall sink to the bottom of the tube; the suitable MOI for infection of HEK293 cells is 5 , calculate the required lentivirus volume according to the number of plated cells and the titer of lentivirus;
[0104] (3) Take out the HEK293 cells from the cell culture incubator, replace them with fresh growth medium, and then add a certain volume of D4 receptor le...
Embodiment 5
[0193] Example 5 is designed as a repeatability test for detecting the biological activity of dopamine D4 target compounds on CHO-K1 / D4 / Nlucp / CRE cells.
[0194] 5.1 Purpose of the experiment Use cryopreserved CHO-K1 / D4 / Nlucp / CRE cells to detect the biological activity of dopamine D4 target compounds, and evaluate the repeatability of the method.
[0195] 5.2 Cell information
[0196]
[0197] 5.3 Experimental steps
[0198] Dopamine agonist and Brilaroxazine (RP5603) adopt the same experimental procedure as in Example 4 to repeat the operation at different time periods and calculate the EC of dopamine agonist and Brilaroxazine 50 ; Wherein Brilaroxazine structural formula is as follows:
[0199]
[0200] 5.4 Results and Analysis
[0201] Table 5: The repeatability evaluation results of the detection method for the biological activity of drugs targeting dopamine D4
[0202] Experiment time DA-D4R EC 50 value
Brilaroxazine EC 50 value
2021091...
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