Attenuation of alcohol-induced hypothermia by cyclo (His-Pro) and its analogs.
Acute administration of cyclo (His-Pro) to rats cause a dose-dependent decrease in ethanol-induced hypothermia. Bromination of the imidazole moiety of histidine in cyclo (His-Pro) resulted in a significant increase in its potency to attenuate ethanol hypothermia. In contrast, benzylation of the imidazole moiety of histidine or the substitution of one or both of the amino acids in cyclo(His-Pro) led to a total loss of its thermomodulatory activity. In conclusion, it appears from these preliminary data that it may be possible to design analogs of CHP that may be effective antagonists for ethanol hypothermia.
Carlton
J
J
Department of Medicine (Section of Endocrinology), Louisiana State University Medical Center, New Orleans, USA.
Khan
S I
SI
Haq
W
W
Mizuma
H
H
Ragan
F A
FA
Mathur
K B
KB
Shukla
R
R
Srimal
R C
RC
Prasad
C
C
D000818:Animals; D001965:Bromides; D000431:Ethanol / Q000008:administration & dosage; D007035:Hypothermia / Q000139:chemically induced* / Q000517:prevention & control*; D008297:Male; D010456:Peptides, Cyclic / Q000737:chemistry / Q000627:therapeutic use*; D010879:Piperazines / Q000737:chemistry / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D001965:Bromides; D010456:Peptides, Cyclic; D010879:Piperazines; C095592:bromo-cyclo(histidyl-prolyl); D000431:Ethanol; C015924:histidyl-proline diketopiperazine