Therapeutic prospects for bradykinin receptor agonists in the treatment of cardiovascular diseases.

摘要

Kinins are located in the vascular smooth muscle and the heart, and are the most potent biologically active polypeptides. Pharmacological studies of cardiovascular disorders, including hypertension, cardiac failure, ischemia, myocardial infarction and left ventricular hypertrophy, indicate that reduced activity of the local kallikrein-kinin system (KKS) may be instrumental in the induction of these disorders. The ability of kallikrein gene delivery and bradykinin (BK) B2 receptor agonists to produce a wide spectrum of beneficial effects make them excellent candidate therapies for the treatment of hypertension, and cardiovascular and renal diseases. In addition, strategies that activate kinin receptors may be applicable to the treatment of cardiovascular and renal disorders. However, one major challenge of this approach is the unanswered question of whether there is a sufficiently safe therapeutic index between the potential cardioprotective and pro-inflammatory effects following administration of BK B2receptor agonists.