Opiates like morphine and endogenous opioid peptides exert their pharmacological and physiological effects through binding to their endogenous receptors, opioid receptors. The opioid receptors are classified into at least three types, mu-, delta- and kappa-types. Recently, cDNAs of the opioid receptors have been cloned and have greatly advanced our understanding of their structure, function and expression. This review focuses on the recent advances in the studies on opioid receptors using the cloned cDNAs. We describe the molecular cloning of the opioid receptor gene family and studies of the structure-function relationships, modes of coupling to second messenger systems, pharmacological effects of antisense oligonucleotide and anatomical distributions of opioid receptors.