[Cyclic analogs of des-Arg9-[Leu8]bradykinin].
Four cyclic derivatives of des-Arg9[Leu8]bradykinin have been obtained by classical methods of peptide chemistry. They are cyclo-(-X-Arg-Pro-Pro-Gly-Phe-Gly-Pro-Leu-), where X=Lys or none, and cyclo-(Y-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Leu-), where Y= Lys or Orn. Peptide bonds have been formed by the pentafluorophenylester method, and cyclization has been carried out in a diluted dioxane solution with 40% yield. Subsequent cleavage of protecting groups was made by treatment with hydrogen fluoride. The products obtained were purified by droplet counter-current chromatography. These substances liberate histamine from the rat mast cells comparably to bradykinin and fail to produce myotripic and vascular effects.
Mutule
I E
IE
Mutulis
F K
FK
Rozite
S Kh
SKh
Porunkevich
E A
EA
Ratkevich
M P
MP
D000595:Amino Acid Sequence; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D002853:Chromatography, Liquid; D006636:Histamine Release / Q000187:drug effects; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D010456:Peptides, Cyclic; D001920:Bradykinin
Tsiklicheskie analogi Dez-Arg9-[Leu8]bradykinina.