[Comparative analysis of analgesic activities of dermorphin, [DPro6]-dermorphin, and their C-terminal tripeptides].
Analgesic activities of dermorphin (DM), [DPro6]-DM, and their C-terminal tripeptides were comparatively studied. Analgesic activity was evaluated in tail flick, hot plate, tail pinch, formalin, and acetic acid writhing tests describing different levels of organization of pain sensitivity. Intraperitoneal administration of the peptides decreased the pain threshold in all these tests. The C-terminal tripeptides DM(5-7) and [DPro6]-DM(5-7) demonstrated analgesics activity comparable or sometimes higher than that of the full-length molecules. The effect of DM, [DPro6]-DM, and C-terminals fragments DM(5-7) and [DPro6]-DM(5-7) decreased after co-administration with naloxone, which points to the opioid nature of analgesic activity of the peptides.
L S
LS
Guzevatykh
T A
TA
Voronina
T G
TG
Emel'ianova
L A
LA
Andreeva
P S
PS
Gromovykh
N F
NF
Miasoedov
S B
SB
Seredenin
D000701:Analgesics, Opioid / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D000818:Animals; D004336:Drug Antagonism; D008297:Male; D051379:Mice; D009270:Naloxone / Q000037:antagonists & inhibitors / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D009842:Oligopeptides / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D018847:Opioid Peptides / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy* / Q000503:physiopathology; D051381:Rats
D000701:Analgesics, Opioid; D009292:Narcotic Antagonists; D009842:Oligopeptides; D018847:Opioid Peptides; C480702:dermorphin, (DPro(6))-; C030058:dermorphin; D009270:Naloxone