Class A GPCRs: Cannabinoid and opioid receptor heteromers

Abstract

Cannabinoid and opioid receptors mediate a variety of physiological processes including pain and drug reward. Both receptors couple to Gαi/o proteins and their activation leads to inhibition of adenylyl cyclase and potassium channel activity ultimately leading to inhibition of synaptic transmission. Over the last decade increasing anatomical, biochemical and pharmacological evidence demonstrated interactions between the opioid and cannabinoid receptor systems that could modulate not only the physiological but also the pathophysiological roles of these receptors. The present review aims to summarize the literature surrounding the properties of cannabinoid and opioid receptors and the unique signaling following their interaction as well as the novel interventions in the management of disorders ranging from pain to addiction.