PubChem: Antagonist of Human D 1 Dopamine Receptor: qHTS

he goal of this project is to use high throughput screening approaches to identify and develop novel, highly selective small molecule allosteric modulators of the D1 DAR for use as in vitro and in vivo pharmacological tools and in proof-of-concept experiments in animal models of neuropsychiatric disease. There are three different types of allosteric modulators that we are seeking, two of which will stimulate or augment receptor signaling, allosteric agonists and potentiators, while the third, allosteric antagonists, will attenuate receptor signaling. The present primary screening assay measures compound antagonism after an EC80 addition of dopamine by tracking calcium flux in a force-coupled, inducible Hek293 Trex D1 cell line.