Pharmacology of amphibian opiate peptides.
In 1980 the skin of certain frogs belonging to the genus Phyllomedusinae was found to contain two new peptides that proved to be selective mu-opioid agonists, and named dermorphins. Since 1987 deltorphins, a family of highly selective delta-opioid peptides were identified either by cloning of the cDNA from frog skins or isolation of the peptides. The distinctive feature of opioid peptides is the presence of a naturally occurring D-enantiomer at the second position in their common N-terminal sequence, Tyr-D-Xaa-Phe. The discovery of the amphibian opiate peptides, provided new insights into the functional role of the mu- and delta-opiate systems. It also provided models for novel analgesics with enhanced therapeutic benefits and reduced toxicity.
Negri
L
L
Department of Human Physiology and Pharmacology, University "La Sapienza," P.le Aldo Moro, 5, I-00185, Rome, Italy. negril@uniroma.it
Melchiorri
P
P
Lattanzi
R
R
D000818:Animals; D002025:Bufonidae; D018076:DNA, Complementary / Q000378:metabolism; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics; D018847:Opioid Peptides; D010455:Peptides / Q000737:chemistry; D017465:Receptors, Opioid, delta / Q000819:agonists / Q000737:chemistry; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000737:chemistry; D012879:Skin Physiological Phenomena; D013329:Structure-Activity Relationship
D018076:DNA, Complementary; D009842:Oligopeptides; D018847:Opioid Peptides; D010455:Peptides; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; C059567:deltorphin; C030058:dermorphin