RABBIT RECOMBINANT B2 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Expression vector containing full-length rabbit B2 cDNA (GenBank Accession Number XM_008249377) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Stability in progress
Background: Bradykinin receptor B2 is a G protein-coupled receptor for bradykinin. Recent studies on mice myocardium revealed that the activation of the cardiac sympathetic system through the stimulation of cardiac sensory nerves involved the activation of the B2 receptor. B2 receptor agonists may have important clinical value in the treatment and prevention of various cardiovascular disorders such as hypertension, ischemic heart disease, left ventricular hypertrophy, ventricular remodeling and congestive heart failure, as well as diabetic disorders by mimicking the reported beneficial effects of bradykinin. Blocking bradykinin B2 receptors after experimental cerebral ischemia reduces brain edema, infarct volume and neuronal necrosis, and improves neurological outcome. Thus, B2 antagonists may be a promising new class of compounds for clinical use after the onset of cerebral ischemia.
Application: Functional assays
Figure 1. Dose-dependent calcium flux upon treatment with ligand, monitored with FLIPR. Figure 2. Dose-dependent increase of intracellular cAMP level upon treatment with ligand. Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Hess et al. (1992) Cloning and pharmacological characterization of a human bradykinin (BK- 2) receptor. Biochem Biophys Res Commun 184:260-268.
Heitsch (2003) The therapeutic potential of bradykinin B2 receptor agonists in the treatment of cardiovascular disease. Expert Opin Investig Drugs 12:759-770.
Jones, W. K., Fan, G.-C., Liao, S., Zhang, J.-M., Wang, Y., Weintraub, N. L., … Ren, X. (2009). Peripheral Nociception Associated With Surgical Incision Elicits Remote Nonischemic Cardioprotection Via Neurogenic Activation of Protein Kinase C Signaling. Circulation, 120(11 Suppl), S1–S9.
Sobey (2003) Bradykinin B2 receptor antagonism: a new direction for acute stroke therapy? Br J Pharmacol 139:1369-1371.