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US 2004/0171080 A1Published application
Method of assaying for agonists or antagonist of dynorphin a binding to the mas receptor
AssigneeAstraZeneca AB
InventorsSultan Ahmad, Eric Grazzini, Paola Lembo
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Abstract
The present invention is directed to assays that can be used to screen for compounds that act as agonists or antagonists or inverse agonists of Dynorphin A and its analogues. The assays are based upon the binding of Dynorphin A and its analogues to the rat and human MAS receptors.
Claims8
A method of assaying a test compound for its ability to bind to the rat and human MAS receptor receptors, comprising:
- a) incubating a cell expressing the MAS receptor gene with Dynorphin A and its analogues, and said test compound;
- and
- b) determining the extent to which the binding of said Dynorphin A and its analogues are displaced by said test compound.
A method of determining if a test compound is an agonist, antagonist or inverse agonist of Dynorphin A and its analogues, comprising:
- a) incubating a cell expressing MAS receptor with said test compounds;
- b) determining the intracellular phospholipase C or adenylyl cyclase activity or intracellular concentration of calcium of said cell during the incubation of step a);
- c) comparing the results obtained in step b) with the results obtained when incubations are performed in the absence of said test compound;
- and
- d) concluding that said test compound are agonist of Dynorphin A and its analogues if the level of phospholipase C or adenyl cyclase activity or intracellular calcium is significantly higher in the presence of said test compounds than in its absence, or concluding that said test compounds are antagonist of Dynorphin A and its analogues if the level of phospholipase C or adenyl cyclase activity or intracellular calcium concentration is significantly lower in the presence of said test compounds than in its absence.
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Dependencies are inferred from the claim text.