[Thermoregulatory activity of dermorphin fragments].
We studied the effect of C-terminal truncation of the dermorphin (DM) molecule and analogs of its N-terminal tetrapeptide, [DOrn2]-DM(1-4), [DArg2]-DM(1-4), [DAla4]-DM(1-4), [DArg2, DAla4]-DM(1-4), Arg-DM(1-4), Arg-[DArg2]-DM(1-4), Arg-[DAla4]-DM(1-4), and Arg-[DArg2, DAla4]-DM(1-4), on the functional status of the thermoregulation system in rats at different ambient temperatures. For the first time, we demonstrate that the N-terminal tetrapeptide is the minimal fragment with the hypothermic effect. Only the N-terminal octapeptide exerted the vasomotor effect. Amino acid substitutions in the tetrapeptide affected its hypothermic effect. [DArg2]-DM(1-4) and [DArg2, DAla4]-DM(1-4) had the greatest effect. Addition of Arg to the N-terminus of DM(1-4) analogs changed their thermoregulatory activity. The greatest thermoregulatory effect was observed for Arg-[DArg2]-DM(1-4) and Arg-[DArg2, DAla4]-DM(1-4).
Emel'ianova
T G
TG
Goriacheva
N N
NN
Guzavatykh
L S
LS
Andreeva
L A
LA
Alfeeva
L Iu
LIu
Miasoedov
N F
NF
D000701:Analgesics, Opioid / Q000008:administration & dosage*; D000818:Animals; D001833:Body Temperature Regulation / Q000187:drug effects* / Q000502:physiology; D008297:Male; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry; D018847:Opioid Peptides; D051381:Rats; D013329:Structure-Activity Relationship
D000701:Analgesics, Opioid; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin