[35S]-GTPγS receptor binding is used to study the distribution and functional activation of neurotransmitter receptors (GPCRs) in tissue sections (rodent, non-human primate & human). This technique combines the advantages of receptor autoradiography and [35S]-GTPγS binding, providing anatomical and functional (EC50 & EMAX) information. Upon binding of an agonist, activated GPCRs can be visualized in the sample.
Functional Receptor Autoradiography can be used to:
- Determine the pharmacological values of potency (EC50) & efficacy (EMAX) of the ligand to activate the GPCR of interest
- Visualize regional differences of activated GPCRs by a ligand
- Determine if the ligand is an agonist or antagonist