FUNCTIONAL ASSAY FOR 5-HT2A RECEPTOR, HISTAMINE H1 RECEPTOR OR ADRENERGIC ALPHA 1B RECEPTOR

摘要

The present invention provides novel functional assay for 5-HT2A, histamine H1 or adrenergic alpha lb receptors, by measuring intracellular cyclic adenosine monophosphate (cAMP) levels utilizing reporter gene driven cell based assay. The novel assay provides both binding affinity as well as mode of action of compounds in a single set. The novel assay of the invention is useful in identification of compounds acting through 5-HT2A, histamine H1 or adrenergic alpha 1b receptors. Furthermore, the assay offers utility in categorizing compounds into agonist, partial agonist, inverse agonist and antagonist classes. The novel assay can be scaled up to any high throughput format.