Biochemical, cellular and pharmacological activities of a human neuropeptide FF-related peptide.
We report on the biochemical, cellular and pharmacological activities of SQA-neuropeptide FF (Ser-Gln-Ala-Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2), a peptide sequence contained in the human neuropeptide FF (neuropeptide FF, Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2) precursor. Quantitative autoradiography revealed that, in the superficial layers of the rat spinal cord, SQA-neuropeptide FF displayed the same high affinity for [125I]1DMe ([125I]D-Tyr-Leu-(NMe)Phe-Gln-Pro-Gln-Arg-Phe-NH2) binding sites (Ki = 0.33 nM) as did neuropeptide FF (Ki = 0.38 nM). In acutely dissociated mouse dorsal root ganglion neurones, SQA-neuropeptide FF reduced by 40% the depolarisation-induced rise in intracellular Ca2+ as measured with the Ca2+ indicator, Fluo-3. In mice, 1DMe and SQA-neuropeptide FF dose-dependently inhibited the antinociceptive effect of intracerebroventricular (i.c.v.) injections of morphine, but SQA-neuropeptide FF was less potent than 1DMe. Furthermore, SQA-neuropeptide FF, as well as 1DMe, produced marked hypothermia following third ventricle injections in mice. These data demonstrate that the human peptide, SQA-neuropeptide FF, exhibits biochemical and pharmacological properties similar to those of neuropeptide FF or neuropeptide FF analogues, and belongs to the neuropeptide FF family.
Gelot
A
A
Institut de Pharmacologie et de Biologie Structurale, CNRS, Toulouse, France.
Mazarguil
H
H
Dupuy
P
P
Francés
B
B
Gouardères
C
C
Roumy
M
M
Zajac
J M
JM
D000701:Analgesics, Opioid / Q000037:antagonists & inhibitors; D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D002118:Calcium / Q000378:metabolism; D005727:Ganglia, Spinal / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007036:Hypothermia, Induced; D008297:Male; D051379:Mice; D009020:Morphine / Q000037:antagonists & inhibitors; D009474:Neurons / Q000187:drug effects / Q000378:metabolism; D009479:Neuropeptides / Q000737:chemistry / Q000494:pharmacology / Q000502:physiology*; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology / Q000502:physiology*; D013116:Spinal Cord / Q000187:drug effects / Q000378:metabolism
D000701:Analgesics, Opioid; D009479:Neuropeptides; D009842:Oligopeptides; C115685:seryl-glutaminyl-alanyl-phenylalanyl-leucyl-phenylalanyl-glutaminyl-prolyl-glutaminyl-arginyl-phenylalaninamide; D009020:Morphine; C053651:phenylalanyl-leucyl-phenylalanyl-glutaminyl-prolyl-glutaminyl-arginyl-phenylalaninamide; D002118:Calcium