[Effect of dermorphin analogs on thermoregulation of rats under various thermal conditions].
We studied the influence of dermorphin (dermorphin) analogs with stereochemical modification of the amino acid residue proline in position 6 (Pro6), Tyr-D-Ala-Phe-Gly-Tyr-Hyp-Ser-NH2, Tyr-D-Ala-Phe-Gly-Tyr-[D-Pro]-Ser-NH2, Tyr-D-Ala-Phe-Gly-Tyr-[dehydro-Pro]-Ser-NH2, and Tyr-D-Ala-Phe-Gly-Tyr-[D-dehydro-Pro]-Ser-NH2, after their intraperitoneal injection at 0.5 mg/kg dose in the cold (4-7 degrees C), thermoneutral (27-28 degrees C), and hot (31-33 degrees C) environment. Stereochemical modifications of amino acid residue Pro6 proved to induce specific changes in the thermoregulatory effect of the peptide. Substitution of DPro6 for Pro6 has the most dramatic consequences: it considerably attenuates the thermoregulatory effect of dermorphin in the cold environment, cancels it in the hot environment, and inverts the dermorphin-specific thermoregulatory response in thermoneutral conditions. The data obtained indicate the important role of Pro6 residue in realization of this physiological activity of dermorphins.
Emel'ianova
T G
TG
Semenov Institute of Chemical Physics, Russian Academy of Sciences, ul. Kosygina 4, Moscow, 119991 Russia. emel@chph.rus.ru
Usenko
A B
AB
Bonartsev
A P
AP
Kamenskiĭ
A A
AA
Guzevatykh
L S
LS
Andreeva
L A
LA
Alfeeva
L Iu
LIu
Miasoedov
N F
NF
D000818:Animals; D021461:Animals, Outbred Strains; D001833:Body Temperature Regulation / Q000187:drug effects*; D003080:Cold Temperature; D006358:Hot Temperature; D008297:Male; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology* / Q000502:physiology; D018847:Opioid Peptides; D011392:Proline / Q000737:chemistry; D051381:Rats; D013329:Structure-Activity Relationship; D013696:Temperature
D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin; D011392:Proline
Vliianie analogov dermorfina na termoreguliatsiiu krys v razlichnykh temperaturnykh rezhimakh.