| Assay Method Information | |
| | Functional Assay |
| Description: | The ability of the compounds to bind and interact with the human H3 receptor as agonists, inverse agonists and/or antagonists, is determined by a functional assay, named [35S]GTPgammaS assay. The assay measures the activation of G proteins by catalyzing the exchange of guanosine 5'-diphosphate (GDP) by guanosine 5' -triphosphate (GTP) at the -subunit. The GTP-bounded G proteins dissociate into two subunits, GGTP and Gbetagamma, which in turn regulate intracellular enzymes and ion channels. GTP is rapidly hydrolysed by the G-sub-unit (GTPases) and the G protein is deactivated and ready for a new GTP exchange cycle. To study the function of ligand-induced G protein coupled receptor (GPCR) activation by an increase in guanine nucleotide exchange at the G proteins, the binding of [35S]-guanosine-5'-O-(3-thio)triphosphate [35S] GTPgamma, a non-hydrolysed analogue of GTP, is determined. |
| Affinity data for this assay | |
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