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
Endogenous opiates and the placebo effect

Refs
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