Lys-(des-Arg9, Leu8)-Bradykinin trifluoroacetate salt is a potent endothelium-dependent vasodilator that causes non-vascular smooth muscle contraction, increases vascular permeability and is also involved in pain mechanisms. Bradykinin also causes an increase in urine sodium, which helps lower blood pressure.

It increases calcium levels inside neocortical astrocytes, causing them to release glutamate.

In some patients treated with angiotensin I-converting enzyme (ACE) inhibitors, bradykinin has been implicated as a cause of dry cough. This difficult-to-treat cough usually results from discontinuation of ACE inhibitor therapy. In such cases, angiotensin II receptor antagonists are used as the next step in therapy.