G-protein coupled receptors (GPCRs) represent by far the largest class of targets for targets for morden drugs. Virtually all therspeutics that are directed towards GPCRs have been designed using assays that presume that these receptors are monomeric. The recent realization that these receptors from homo-oligomeric and heteroligomeric complexs has added a new dimension to rational drug design. However, this important aspect of GPCR biology remains largely unincorporated into schemes to search for new therapetics. This review provides a synopsis of the current thinking surrounding GPCR homooligomerization and heterooligomerization and shows how new models point towards unexplored avenues in the development of new therapies.