Mu opioids and their receptors: Evolution of a concept Journal Article
| Authors: | Pasternak, G. W.; Pan, Y. X. |
| Article Title: | Mu opioids and their receptors: Evolution of a concept |
| Abstract: | Opiates are among the oldest medications available tomanage a number of medical problems. Although pain is the current focus, early use initially focused upon the treatment of dysentery. Opium contains high concentrations of both morphine and codeine, along with thebaine, which is used in the synthesis of a number of semisynthetic opioid analgesics. Thus, it is not surprising that new agents were initially based upon the morphine scaffold. The concept of multiple opioid receptors was first suggested almost 50 years ago (Martin, 1967), opening the possibility of new classes of drugs, but the morphine-like agents have remained the mainstay in the medical management of pain. Termed mu, our understanding of these morphine-like agents and their receptors has undergone an evolution in thinking over the past 35 years. Early pharmacological studies identified three major classes of receptors, helped by the discovery of endogenous opioid peptides and receptor subtypes- primarily through the synthesis of novel agents. These chemical biologic approaches were then eclipsed by the molecular biology revolution, which now reveals a complexity of the morphine-like agents and their receptors that had not been previously appreciated. © 2013 by The American Society for Pharmacology and Experimental Therapeutics. |
| Keywords: | immunohistochemistry; unclassified drug; promoter region; single nucleotide polymorphism; exon; constipation; review; drug penetration; nonhuman; unindexed drug; pain; opiate; qt prolongation; genetic variability; drug potency; drug structure; drug synthesis; structure activity relation; central nervous system; drug receptor binding; pethidine; drug mechanism; bioassay; alternative rna splicing; cellular distribution; temperature; drug dependence; drug blood level; methadone; morphine; respiration depression; molecular biology; drug binding site; hydromorphone; analgesia; drug tolerance; digestive system function disorder; mu opiate receptor; tail flick test; naloxone; knockout gene; chromosome map; fentanyl; diamorphine; morphine 6 glucuronide; naltrindole; naltrexone; analgesic activity; levorphanol; phylogeny; codeine; buprenorphine; dynorphin a; naloxonazine; levallorphan; drug cross tolerance; butorphanol; ketazocine; morphinan derivative; etonitazene; naloxazone; human; priority journal; 14 hydroxymetopon; benzomorphan derivative; diprenorphine; etorphine; meptazinol; nalorphine |
| Journal Title: | Pharmacological Reviews |
| Volume: | 65 |
| Issue: | 4 |
| ISSN: | 0031-6997 |
| Publisher: | The American Society for Pharmacology and Experimental Therapeutics |
| Date Published: | 2013-10-01 |
| Start Page: | 1257 |
| End Page: | 1317 |
| Language: | English |
| DOI: | 10.1124/pr.112.007138 |
| PROVIDER: | scopus |
| PMCID: | PMC3799236 |
| PUBMED: | 24076545 |
| DOI/URL: | |
| Notes: | Cited By (since 1996):6 -- Export Date: 9 May 2014 -- CODEN: PAREA -- Source: Scopus |
Altmetric
Citation Impact
BMJ Impact Analytics
Related MSK Work