| Abstract: | 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-Glycyclo (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. |
