Vasopressin analogs of the formula <IMAGE> wherein R1 is H, R2 is CH2S and R3 is D-Arg, R1 is NH2, R2 is S-S and R3 is D-Arg or L-Orn are described. The described analogs resist enzymatic cleavage while retaining their effect on the central nervous system. These compounds lack a glycinamide residue in the 9 position and have the L-arginine in the 8 position replaced with its stereoisomeric form or with an ornithine residue. The compounds evidence little or no peripheral endocrine effects of natural vasopressin.
申请公布号
US4482486(A)
申请公布日期
1984.11.13
申请号
US19830486863
申请日期
1983.04.20
申请人
CESKOSLOVENSKA AKADEMIE VED
发明人
BRTNIK, FRANTISEK;BARTH, TOMISLAV;HRBAS, PAVEL;JOST, KAREL;KREJCI, IVAN;KUPKOVA, BELA;MACHOVA, ALENA;SERVITOVA, LINDA;SKOPKOVA, JANA