Mu Opioid Receptor Bound to a Morphinan Antagonist

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Introduction and Background Information

Opium is one of the oldest drugs known to mankind and still has prevalence today. Morphine and codeine, two opiate products, are heavily used both in clinical settings and illegally to to control pain and produce analgesic and unwanted side effects. Mu-opioid receptors are a group of G-protein-coupled receptors and have been found to be the target for the majority of effects of opioid alkaloids.[1] There are 17 known opioid receptors with the three primary types being the μ, κ, and δ. The μ opioid receptor (μ-OR) is the most related to opioid use. There are three subtypes μ1, μ2, μ3 and most is known about μ1.[2] The μ-ORs are part of the neurohormonal system. Within the body (sans drugs) endogenous small molecules naturally produced in the CNS and other glands act upon the GPCRs. Endogenous opioid peptides produce can range in action from pain reduction to regulating diarrhea.[3]

Crystal structure of the mu-opioid receptor bound to a morphinan antagonist, cholesterol, PEG 400, sulfate, mono-oleoyl-glycerol and Cl- ion (PDB entry 4dkl)

Proteopedia Page Contributors and Editors (what is this?)

Greg Angelides, Karsten Theis, Michal Harel, Wayne Decatur

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