[Biologically active loop-shaped analogs of bradykinin and polisteskinin].
The classical methods of peptide chemistry have been employed to synthesize loop-shaped derivatives of bradykinin and polisteskinin, Lys-Lys-Lys-[cyclo (9----1 epsilon), Lys1, Gly6]bradykinin and Lys-Lys-Lys-Leu-Arg-Gly[cyclo (9----1 epsilon)Lys1, Gly6] bradykinin. In the course of synthesis, the linear "tail" fragments were attached to partially deblocked cyclopeptide. Protective groups were removed by treating with hydrogen fluoride, the end products were purified using reversed-phase and ion exchange chromatography. Biological experiments in vivo have revealed that the two compounds elicit a prolonged hypotensive effect in rats which is characteristic of cyclic bradykinin analogues. With the latter compound, a decrease in arterial pressure is preceded by a brief hypertensive action. The loop-shaped analogues are slightly myotropic when applied to rat uterus preparations in vitro.
D000818:Animals; D001514:Bee Venoms / Q000138:chemical synthesis*; D001794:Blood Pressure / Q000187:drug effects; D001920:Bradykinin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D005260:Female; D066298:In Vitro Techniques; D010455:Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D014590:Uterine Contraction / Q000187:drug effects; D014862:Wasp Venoms / Q000138:chemical synthesis* / Q000494:pharmacology
D001514:Bee Venoms; D010455:Peptides; D014862:Wasp Venoms; C043415:polisteskinin; D001920:Bradykinin
Biologicheski aktivnye petleobraznye analogi bradikinina i polisteckinina.