. 2016 Sep 8;7(10):956–961. doi: 10.1021/acsmedchemlett.6b00290

Table 1. Binding Affinity (pK_i^a) at I₁- and I₂-IBS on Rat Brain Membranes; Binding Affinity (pK_i^a), Antagonist Potency (pK_b^b), Agonist Potency (pEC₅₀^b), and Intrinsic Activity (ia^b) at Human α₂-Adrenergic Receptors Subtypes on CHO Cells.

graphic file with name ml-2016-002903_0006.jpg

pK_i affinity values for I₁-IBS, I₂-IBS, and α₂-ARs were assessed by measuring the ability of the tested compounds to displace [¹²⁵I]-p-iodoclonidine (rat kidney membranes), [³H]-2-BFI (rat brain membranes), and [³H]-RX 821002 (rat brain membranes), respectively.

pK_b, pEC₅₀, and ia values were determined by applying the Cytosensor microphysiometry system to the CHO cells expressing individual each human α₂-AR subtype. Intrinsic activity of the tested compounds is expressed as the fraction of that of the full agonist (−)-noradrenaline taken as equal to 1. The data are expressed as mean ± SEM of 3–5 separate experiments.

Reference (21).

References (22) and (23).

Re-examined in the experimental conditions of the present study.

Table 1. Binding Affinity (pKia) at I1- and I2-IBS on Rat Brain Membranes; Binding Affinity (pKia), Antagonist Potency (pKbb), Agonist Potency (pEC50b), and Intrinsic Activity (iab) at Human α2-Adrenergic Receptors Subtypes on CHO Cells.

Table 1. Binding Affinity (pK_i^a) at I₁- and I₂-IBS on Rat Brain Membranes; Binding Affinity (pK_i^a), Antagonist Potency (pK_b^b), Agonist Potency (pEC₅₀^b), and Intrinsic Activity (ia^b) at Human α₂-Adrenergic Receptors Subtypes on CHO Cells.