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. 2005 Oct 19;7(3):E587–E591. doi: 10.1208/aapsj070360

Mu opioid receptor regulation and opiate responsiveness

Kirsten M Raehal 1, Laura M Bohn 1,✉
PMCID: PMC2751262  PMID: 16353937

Abstract

Opiate drugs such as morphine are well known for their ability to produce potent analgesia as well as such unwanted side effects as tolerance, physical dependence, respiratory suppression and constipation. Opiates act at opioid receptors, which belong to the family of G protein-coupled receptors. The mechanisms governing mu opioid receptor (μOR) regulation are of particular interest since morphine and other clinically important analgesics produce their pharmacological effects through this receptor. Here we review recent advances in understanding how opioid receptor regulation can impart differential agonist efficacy produced in vivo.

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