Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitory activity on B2 receptors[1][2].
Lys-[Des-Arg9]Bradykinin is formed by the proteolytic cleavage of bradykinin, exerts its effects through bradykinin B1 receptor (B1R)[1].Lys-[Des-Arg9]Bradykinin (Lda-BK; 10 μM) enhances the secretion of IL-12p70 and inhibits the secretion of IL-12p40 by mature hMo-DCs. Pretreatment with Lys-[Des-Arg9]Bradykinin treatment reduces the migration of mature hMo-DCs toward medium alone, suggesting that Lys-[Des-Arg9]Bradykinin may inhibit the chemokinesis of mature hMo-DCs[1].
Lys-[Des-Arg9]Bradykinin (1 μg; intra-artenal injection; New Zealand White rabbits) treatment reduces peripheral vascular resistance in LPS-induced rabbits, but the effect is brief (T1/2 is 118-195 s)[3].
[1]. Rosalind Gulliver, et al. Lys-des[Arg9]-bradykinin alters migration and production of interleukin-12 in monocyte-derived dendritic cells. Am J Respir Cell Mol Biol. 2011 Sep;45(3):542-9. [2]. L M Fredrik Leeb-Lundberg, et al. International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol Rev. 2005 Mar;57(1):27-77. [3]. G Drapeau, et al. Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kinins. J Pharmacol Exp Ther. 1991 Dec;259(3):997-1003.