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