Opioids and their receptors: Are we there yet?

摘要: Opioids have an important place in pharmacology. While their clinical use as analgesics is fundamental medicine, constrained by side-effects and abuse potential. Pharmacologists sought lacking the liability of current agents. The identification opioid receptors 1973 marked beginning our understanding molecular mechanisms these isolation peptides quickly followed, along with classification three families receptors. Clinicians long been aware subtle differences among mu opioids that were not easily reconciled a single receptor selective antagonists implied two subdivisions However, cloning MOR-1 has led to realization extensive complexity gene its vast array splice variants. Many variants are truncated do conform structure traditional G-protein coupled Yet, evidence now shows they quite may prove valuable targets development potent undesirable properties opioids. This article part Special Issue entitled 'NIDA 40th Anniversary Issue'.