Identification of ligands by selective amplification of cells transfected with receptors
AssigneeACADIA Pharmaceuticals Inc.
InventorMark R. Brann
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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.
Claims22
A method of alleviating symptoms in a patient with a disease or disorder associated with constitutive activity of 5-HT2A receptor, comprising administering an antipsychotic and a 5-HT2A selective inverse agonist to the patient.
A method of reducing extrapyramidal side effects associated with administration of antipsychotic drugs to a patient with symptoms of a disease or disorder associated with constitutive activity of 5-HT2A receptor, comprising administering an effective dose of a 5-HT2A selective inverse agonist to said patient.
A method of reducing the effective dosage of an antipsychotic drug needed to treat symptoms of a disease or disorder associated with constitutive activity of 5-HT2A receptor in a patient, comprising administering an effective dose of a 5-HT2A selective inverse agonist to said patient in combination with said antipsychotic drug.
A pharmaceutical composition comprising a 5-HT2A selective inverse agonist and an antipsychotic.
Dependencies are inferred from the claim text.