Overview
- Davenport, A.P. et al. (1998) Br. J. Pharmacol. 123, 223.
Alomone Labs PD-164333 inhibits ETA receptor-mediated Ca2+ mobilization in CHO-K1 cells.Dose response curve of PD-164333 (#P-310) inhibition of the ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 7.59 nM.
Cells were loaded with Calcium 6 dye, incubated with PD164333, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
PD-164333 is a synthetic compound that acts as a selective antagonist of ET-A endothelin receptor based on the butenolide series1. It inhibits the binding of radioligand endothelin-1 to left ventricle in a biphasic manner with a KD value of 0.99 nM and 2.41 µM towards ET-A and ET-B, respectively1.
Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in different regions of the brain. ET-A receptor has a high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity equally for all endothelin isopeptides2.
