Identification of ligands by selective amplification of cells transfected with receptors
First Claim
1. A method of determining whether a substance is a ligand of a receptor, said method comprising:
- obtaining a first population of cells comprising said receptor, wherein DNA encoding a marker indicative of the extent of cellular proliferation has been introduced into said first population of cells and wherein the amount of marker in said cells is influenced by the degree to which said receptor is active;
contacting said first population of cells with a test substance which is a potential ligand of said receptor;
comparing the amount of marker in said first population of cells which has been contacted with said test substance to the amount of marker in a second population of cells which has not been contacted with said test substance, said second population of cells comprising said receptor and DNA encoding said marker such that the extent of marker activity in said cells is influenced by the degree to which said receptor is active, wherein said test substance is a ligand of said receptor if the amount of marker in said first population of cells is significantly different than the amount of marker in said second population of cells.
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Abstract
The invention is directed to a method for identifying substances acting as ligands for transfected receptors by using transfected markers to measure receptor/ligand interactions. The present invention also relates to a method of identifying compounds which act as inverse agonists of the 5-HT2A receptor, the method comprising contacting a constitutively active 5-HT2A receptor with at least one test compound and determining any decrease in the amount of basal activity of the receptor so as to identify a test compound which is an inverse agonist of the 5-HT2A receptor. Such inverse agonists may be used in the treatment of schizophrenia and related psychoses.
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Citations
10 Claims
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1. A method of determining whether a substance is a ligand of a receptor, said method comprising:
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obtaining a first population of cells comprising said receptor, wherein DNA encoding a marker indicative of the extent of cellular proliferation has been introduced into said first population of cells and wherein the amount of marker in said cells is influenced by the degree to which said receptor is active;
contacting said first population of cells with a test substance which is a potential ligand of said receptor;
comparing the amount of marker in said first population of cells which has been contacted with said test substance to the amount of marker in a second population of cells which has not been contacted with said test substance, said second population of cells comprising said receptor and DNA encoding said marker such that the extent of marker activity in said cells is influenced by the degree to which said receptor is active, wherein said test substance is a ligand of said receptor if the amount of marker in said first population of cells is significantly different than the amount of marker in said second population of cells. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
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Specification