Methods for detecting receptor modulator activity
First Claim
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1. A high-throughput method for identifying partial agonists and partial antagonists of a G-protein coupled receptor, the method comprising the steps ofa) contacting, at a temperature of about 25°
- C., a test compound with a cell expressing the receptor;
b) detecting a change in the level of activity of the receptor;
c) contacting, at a temperature of about 35°
C., a test compound with a cell expressing the receptor;
d) detecting a change in the level of activity of the receptore) comparing the result obtained in step b) with the result obtained in step d) wherein a partial agonist or antagonist of the G-protein coupled receptor is identified if a compound shows no activity at a temperature of about 25°
C. but does show activity at a temperature of about 37°
C.
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Abstract
Disclosed herein are methods of screening compounds that modulate G-protein coupled receptors. The assays are performed at temperatures of between about 25° C. and 40° C.
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4 Claims
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1. A high-throughput method for identifying partial agonists and partial antagonists of a G-protein coupled receptor, the method comprising the steps of
a) contacting, at a temperature of about 25° - C., a test compound with a cell expressing the receptor;
b) detecting a change in the level of activity of the receptor; c) contacting, at a temperature of about 35°
C., a test compound with a cell expressing the receptor;d) detecting a change in the level of activity of the receptor e) comparing the result obtained in step b) with the result obtained in step d) wherein a partial agonist or antagonist of the G-protein coupled receptor is identified if a compound shows no activity at a temperature of about 25°
C. but does show activity at a temperature of about 37°
C. - View Dependent Claims (2, 3, 4)
- C., a test compound with a cell expressing the receptor;
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