Historical review: Opioid receptors Journal Article


Authors: Snyder, S. H.; Pasternak, G. W.
Article Title: Historical review: Opioid receptors
Abstract: A historical review of the early phases of molecular investigations of opioid receptors is presented. The 'modern' era of molecular studies of neurotransmitter and drug receptor research commenced in the 1970s with the identification of receptors using ligand binding techniques. These findings had several ramifications. Reversible ligand binding to opioid receptors using simple, sensitive and specific techniques provided a paradigm for the study of receptors for the principal neurotransmitters in the brain. The relatively high-throughput binding techniques employed facilitated drug development in the pharmaceutical industry. Differentiation of agonist and antagonist receptor interactions by Na+ ions and other substances helped elucidate how ligand recognition at receptors is translated into second messenger alterations. Localizations of opioid receptors clarified many of the pharmacological actions of opiate drugs. Differential binding interactions of various drugs led to the identification of opioid receptor subtypes. Receptor influences in binding paradigms and smooth muscle pharmacology permitted the identification and isolation of endogenous opioid peptides.
Keywords: unclassified drug; drug activity; review; nonhuman; binding affinity; protein function; protein localization; animals; history, 20th century; pethidine; drug mechanism; binding site; methadone; morphine; g protein coupled receptor; ligand binding; naloxone; opiate receptor; naltrexone; levorphanol; drug industry; second messenger; receptor subtype; codeine; oxymorphone; cyclazocine; pentazocine; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; proopiomelanocortin; dextropropoxyphene; leucine enkephalin; opiate peptide; neurotransmitter; levallorphan; portraits; sodium ion; naltrexone derivative; receptors, opioid; calcium channel; phenazocine; humans; priority journal; diprenorphine; etorphine; nalorphine; dihydromorphine; 3 methylnaltrexone; dextrorphan; metenkephalin
Journal Title: Trends in Pharmacological Sciences
Volume: 24
Issue: 4
ISSN: 0165-6147
Publisher: Cell Press  
Date Published: 2003-04-01
Start Page: 198
End Page: 205
Language: English
DOI: 10.1016/s0165-6147(03)00066-x
PUBMED: 12707007
PROVIDER: scopus
DOI/URL:
Notes: Export Date: 25 September 2014 -- Source: Scopus
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  1. Gavril W Pasternak
    414 Pasternak