A synthetic peptide as an antagonist of substance P

The undecapeptide substance P (SP) is believed to participate in synaptic transmission in primary sensory neurones and in many other parts of the central nervous system 1,2 , including (in the rat) the pontine structure locus coeruleus (LC). So far, studies of the role of SP in the central nervous s...

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Bibliographic Details
Published in:Nature (London) 1981-09, Vol.293 (5829), p.222-223
Main Authors: Engberg, Göran, Svensson, Torgny H, Rosell, Sune, Folkers, Karl
Format: Article
Language:English
Subjects:
Acetylcholine - pharmacology
Action Potentials - drug effects
Animals
Glutamates - pharmacology
Glutamic Acid
Humanities and Social Sciences
letter
Locus Coeruleus - physiology
Male
multidisciplinary
Rats
Rats, Inbred Strains
Science
Science (multidisciplinary)
Substance P - analogs & derivatives
Substance P - antagonists & inhibitors
Substance P - pharmacology
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Summary:The undecapeptide substance P (SP) is believed to participate in synaptic transmission in primary sensory neurones and in many other parts of the central nervous system 1,2 , including (in the rat) the pontine structure locus coeruleus (LC). So far, studies of the role of SP in the central nervous system have been impeded by the lack of a specific antagonist to SP. Immunoneutralization of SP has been used 3 , and more recently synthetic analogues of SP, in which D -amino acids are substituted for L-amino acids, have been found to block peripheral effects of SP 4,5 . We now describe experiments which show that the peptide which differs from SP in the presence of D -Pro at position 2 and D -Trp at positions 7 and 9 specifically blocks in vivo the SP-induced excitation of LC neurones and is thus a CNS antagonist of SP.
ISSN:0028-0836
1476-4687
DOI:10.1038/293222a0