Biotin-linked bradykinin was synthesized by solid phase peptide synthesis for development of a functionalized peptide and study on structure-relevant bioactivity in biological system. In PC12 cell system, bioactivity of the synthetic peptide was evaluated and found to be controllable in the presence of neutravidin and free biotin. The controlling mechanism had been discussed and could be ascribed to steric hindrance induced by binding of neutravidin to the linked biotin. Moreover, influence of competitive binding between the free biotin and the linked biotin to the neutravidin had also investigated into and could be employed for switching the bioactivity on and off.