Description
Lys-(Des-Arg9)-Bradykinin is a naturally occurring peptide agonist of the bradykinin B1 receptor (Ki = 0.12 nM in HEK293 cells expressing the human receptor).1,2 It is selective for bradykinin B1 over B2 receptors (IC50 = >30,000 nM in CHO cells expressing the human receptor).3 Lys-(Des-Arg9)-Bradykinin increases both mRNA and protein levels of the B1 receptor in IMR-90 human lung fibroblasts in a concentration-dependent manner.4 It induces contraction of isolated rabbit aorta (pD2 = 8.6).5 Lys-(Des-Arg9)-Bradykinin decreases blood pressure in LPS-treated rabbits in a dose-dependent manner.2WARNING This product is not for human or veterinary use.
References
[1] S. BASTIAN. Stable expression of human kinin B1 receptor in 293 cells: pharmacological and functional characterization[J]. British Journal of Pharmacology, 2009, 122 2: 393-399. DOI: 10.1038/sj.bjp.0701380
[2] G DRAPEAU F M D deBlois. Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kinins.[J]. Journal of Pharmacology and Experimental Therapeutics, 1991, 259 3: 997-1003.
[3] J F HESS. Differential pharmacology of cloned human and mouse B2 bradykinin receptors.[J]. Molecular Pharmacology, 1994, 45 1: 1-8.
[4] J P SCHANSTRA. The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the bradykinin B1-receptor in cultured human lung fibroblasts.[J]. Journal of Clinical Investigation, 1998, 101 10: 2080-2091. DOI: 10.1172/jci1359
[5] NOUR-EDDINE RHALEB. Structure-activity studies on bradykinin and related peptides: agonists[J]. British Journal of Pharmacology, 1990, 99 3: 445-448. DOI: 10.1111/j.1476-5381.1990.tb12947.x
