Table 1 of
Sharif, Mol Vis 2013; 19:1356-1370.
Table 1. Functional agonist and antagonist potencies at primary h-CM cell B2-receptor compared with h-TM cell responses, and ligand binding to human cloned B2-receptors
Compound | Agonist Potency at stimulating [Ca2+]i mobilization in primary h-CM cells (EC50, nM) | Agonist Potency at stimulating [Ca2+]i mobilization in primary h-TM cells (EC50, nM) | Ligand binding inhibition constant at human cloned B2 receptors (Ki, nM) |
---|---|---|---|
Agonists | |||
Hyp3-BK | 2.2±0.2 | 1 | 1.9±1.1 |
BK | 2.4±0.2 | 1 | 0.5±0.01 |
Lys-BK | 3.2±0.8 | 2 | 1.8±0.7 |
RMP-7 | 3.7±1.2 | nd | 11.3±1.1 |
Met-Lys-BK | 16.1±6.1 | 7 | 73.0±24.7 |
Des-Arg9-BK | 4,200±570 | 3,600 | 10,400±5,900 |
Antagonists blocking the actions of BK or competing for [3H]-BK binding to B2-receptor | Antagonist potency (IC50, nM) | Antagonist potency (IC50, nM) | Ligand binding inhibition constant at human cloned B2 receptors (Ki, nM) |
HOE-140 | 1.4±0.1 | 5 | 0.5±0.2 |
(S)-WIN-64338 | 174±18 | 270 | 170.0±52.2 |