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The μ opioid receptor: from molecular cloning to functional studies
Author(s) -
YU LEI
Publication year - 1996
Publication title -
addiction biology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.445
H-Index - 78
eISSN - 1369-1600
pISSN - 1355-6215
DOI - 10.1080/1355621961000124666
Subject(s) - opioid , morphine , adenylyl cyclase , heroin , pharmacology , opioid receptor , euphoriant , receptor , chemistry , fentanyl , neuroscience , medicine , biology , biochemistry , drug
Opioids have been used and abused by humans for centuries. The μ opioid receptor represents the high affinity binding site for opioid narcotics with high abuse liability such as morphine, codeine and fentanyl. Heroin (diacetylmorphine), a semi‐synthetic derivative of morphine, crosses the blood‐brain barrier more readily than morphine due to its increased hydrophobicity. Once in the brain heroin is hydrolyzed to morphine, which acts at the μ opioid receptor and results in euphoria, thus conferring the reinforcing properties of heroin. Using molecular biology techniques, the μ opioid receptors from several species have been cloned. This article reviews recent progress in this area, with respect to the two major cellular functions of the μ opioid receptor: reduction of intracellular cAMP concentration by inhibiting adenylyl cyclase activity, and inhibition of neuronal firing by modulating membrane ion channels.