Synthesis and analgesic effects of kyotorphin-steroid linkers.
Kyotorphin (KTP, H-Tyr-Arg-OH) was covalently bonded with hydrocortisone or estrone to form the corresponding hydrocortisone-21-O-yl-succinyl-Tyr-ArgOH or estrone-3-O-yl-acyl-Tyr-Arg-OH. Their analgesic activities were investigated using the tail flick test. The potency of the two linkers were significantly higher than that of KTP and the mixture of KTP and hydrocortisone or estrone in the CNS and/or the periphery administration.
Wang
C
C
College of Pharmaceutical Sciences, Peking University, Beijing 100083, P.R. China.
Zhao
M
M
Yang
J
J
Peng
S
S
D000700:Analgesics / Q000008:administration & dosage* / Q000138:chemical synthesis; D000818:Animals; D002417:Cattle; D002490:Central Nervous System / Q000187:drug effects; D004723:Endorphins / Q000737:chemistry; D004970:Estrone / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D006854:Hydrocortisone / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D017288:Pain Threshold / Q000187:drug effects*; D017933:Peripheral Nervous System / Q000187:drug effects; D051381:Rats
D000700:Analgesics; D004723:Endorphins; C441512:estrone-3-O-yl-acyl-Tyr-Arg-OH; C441511:hydrocortisone-21-O-yl-succinyl-Tyr-ArgOH; C019448:kyotorphin; D004970:Estrone; D006854:Hydrocortisone