From Opiate Pharmacology to Opioid Peptide Physiology

  • Lars Terenius Experimental Alcohol and Drug Addiction Section, Department of Clinical Neuroscience, Karolinsku Institutet, S-I71 76 Stockholm, Sweden


This is a personal account of how studies of the pharmacology of opiates led to the discovery of a family of endogenous opioid peptides, also called endorphins. The unique pharmacological activity profile of opiates has an endogenous counterpart in the enkephalins and β-endorphin, peptides which also are powerful analgesics and euphorigenic agents. The enkephalins not only act on the classic morphine (μ-) receptor but also on the δ-receptor, which often co-exists with μ-receptors and mediates pain relief. Other members of the opioid peptide family are the dynorphins, acting on the κ-receptor earlier defined as precipitating unpleasant central nervous system (CNS) side effects in screening for opiate activity. A related peptide, nociceptin is not an opioid and acts on the separate NOR-receptor. Both dynorphins and nociceptin have modulatory effects on several CNS functions, including memory acquisition, stress and movement. In conclusion, a natural product, morphine and a large number of synthetic organic molecules, useful as drugs, have been found to probe a previously unknown physiologic system. This is a unique development not only in the neuropeptide field, but in physiology in general.


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How to Cite
Terenius L. (2000). From Opiate Pharmacology to Opioid Peptide Physiology. Upsala Journal of Medical Sciences, 105(1), 1-16.
Original Articles