From opiate pharmacology to
opioid peptide physiology
by
Terenius L Department of Clinical Neuroscience,
Karolinska Institutet,
Stockholm,
Sweden.
Ups J Med Sci 2000; 105(1):1-15

ABSTRACT

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 beta-endorphin, peptides which also are powerful analgesics and euphorigenic agents. The enkephalins not only act on the classic morphine (mu-) receptor but also on the delta-receptor, which often co-exists with mu-receptors and mediates pain relief. Other members of the opioid peptide family are the dynorphins, acting on the kappa-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.

Pain
LAAM
Arousal
Morphine
Tramadol
Nociceptin
Methadone
Endomorphins
P-glycoprotein
Morphine worms
Novelty and pain
Discounting rewards
Fentanyl and ketamine
Opioids, mood and cognition
Opioids, dopamine and alcohol
Opioids, goldfish and the giant toad

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