<p><i>n</i> represents the number of experiments, each performed in triplicate.</p><p>Ø represents no binding at concentrations up to 100 µM.</p>a<p>p<i>K</i><sub>i</sub> (−Log <i>K</i><sub>i</sub>).</p>b<p><i>K</i><sub>i</sub> (inhibition constants) are the antilog of mean p<i>K</i><sub>i</sub>.</p><p><i>K</i><sub>i</sub> values were calculated according to the equation of Cheng and Prusoff . <i>K</i><sub>i</sub> = IC<sub>50</sub>/1 + ([L]/<i>K</i><sub>D</sub>) when [L] is the radioligand concentration and <i>K<sub>D</sub></i> its dissociation constant.</p>A<p>indicates significant differences from the α<sub>1A</sub> –AR (<i>p</i><0.05).</p>B<p>indicates significant differences from the α<sub>1B</sub> –AR (<i>p</i><0.05).</p>D<p>indicates...
Abstract Highly selective drugs offer a way to minimize side‐effects. For agonist ligands, this coul...
In this study, we report the beta1-adrenoceptor binding kinetics of several clinically relevant beta...
α1 adrenoceptors are three of the nine receptors that bind and respond to the hormones adrenali...
AbstractKinetic on and off rate constants for many receptor ligands are difficult to determine with ...
Kinetic on and off rate constants for many receptor ligands are difficult to determine with regular ...
<p>The competitive displacement of the non-selective radiolabeled antagonist (<sup>125</sup>I)-cyano...
<p><b><i>A</i></b>. Competitive displacement of a non-selective antagonist radioligand from a mixed ...
Adrenergic receptors (ARs) are members of the super family of G protein-coupled receptors (GPCRs). A...
<p><b><i>A</i></b>. Proof-of-concept saturation experiments with β<sub>1</sub>AR-overexpressing memb...
<p>The competitive displacement of the non-selective radiolabeled antagonist <b>(</b><sup>125</sup>I...
β2-Adrenoceptor selectivity is an important consideration in drug design in order to minimize the po...
Measuring the rate and extent of radioligand binding provides information on the number of binding s...
The structural poses of ligands that bind weakly to protein receptors are challenging to define. In ...
α<sub>1A</sub>- and α<sub>1B</sub>-adrenoceptors (α<sub>1A</sub>-AR and α<sub>1B</sub>-AR) are close...
Biomedical applications of molecules that are able to modulate β-adrenergic signaling have become in...
Abstract Highly selective drugs offer a way to minimize side‐effects. For agonist ligands, this coul...
In this study, we report the beta1-adrenoceptor binding kinetics of several clinically relevant beta...
α1 adrenoceptors are three of the nine receptors that bind and respond to the hormones adrenali...
AbstractKinetic on and off rate constants for many receptor ligands are difficult to determine with ...
Kinetic on and off rate constants for many receptor ligands are difficult to determine with regular ...
<p>The competitive displacement of the non-selective radiolabeled antagonist (<sup>125</sup>I)-cyano...
<p><b><i>A</i></b>. Competitive displacement of a non-selective antagonist radioligand from a mixed ...
Adrenergic receptors (ARs) are members of the super family of G protein-coupled receptors (GPCRs). A...
<p><b><i>A</i></b>. Proof-of-concept saturation experiments with β<sub>1</sub>AR-overexpressing memb...
<p>The competitive displacement of the non-selective radiolabeled antagonist <b>(</b><sup>125</sup>I...
β2-Adrenoceptor selectivity is an important consideration in drug design in order to minimize the po...
Measuring the rate and extent of radioligand binding provides information on the number of binding s...
The structural poses of ligands that bind weakly to protein receptors are challenging to define. In ...
α<sub>1A</sub>- and α<sub>1B</sub>-adrenoceptors (α<sub>1A</sub>-AR and α<sub>1B</sub>-AR) are close...
Biomedical applications of molecules that are able to modulate β-adrenergic signaling have become in...
Abstract Highly selective drugs offer a way to minimize side‐effects. For agonist ligands, this coul...
In this study, we report the beta1-adrenoceptor binding kinetics of several clinically relevant beta...
α1 adrenoceptors are three of the nine receptors that bind and respond to the hormones adrenali...