Both natural and synthetic peptides displayed a selective potentiating activity on isolated guinea-pig ileum for bradykinin and Lys-bradykinin but were not able to potentiate the effects of Met-Lys-bradykinin, Ile-Ser-bradykinin, angiotensin II, acetylcholine, or histamine. This bradykinin-potentiating octapeptide is a strong competitive inhibitor of endo-oligopeptidase A (EC 3.4.24.15, formerly EC 3.4.22.19), but it has low inhibitory potency towards angiotensin-converting enzyme (EC 3.4.15.1).
Table 1. Bradykinin-potentiating effects of CBPP (natural and synthetic) on the isolated guinea-pig ileum and isolated rat uterus.
Assay
| Potentiator
| Concn. for 1 unit of potentiationa (ng/mL)
| Relative activity
| Isolated guinea-pig ileum
| CBPP (natural)
| 10.8
| 1
| CBPP (Synthetic)
| 11.5
| 1.1
| Potentiator B
| 2791
| 0.004
| BPP5a
| 490
| 0.02
| AVI-5
| 16405
| 0.0006
| NOTEA: All potentiators were tested in the presence of 2 ng/mL bradykinin in the bath. a 1 unit of potentiation = twofold increase of ileum or uterus contraction for a constant bradykinin dose. The standard errsr for these values was less than 5%. | |