Related Experiment Video
Updated: Aug 29, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors
Ben D Popp1, Dana S Hutchinson, Bronwyn A Evans
1Department of Pharmacology, Monash University, Victoria 3800, Australia.
Abstract:
This study examines the stereoselectivity profile of recombinant mouse, rat and human beta(3)-adrenoceptors expressed in Chinese Hamster Ovary (CHO-K1) cells using radioligand binding, in comparison with endogenously expressed beta(3)-adrenoceptors mediating relaxation responses in mouse ileum. The enantiomeric ratios for several beta-adrenoceptor agonists and antagonists at the cloned mouse, rat and human beta(3)-adrenoceptor were less than those reported at the cloned beta(1)-/beta(2)-adrenoceptor but higher than those reported in previous studies. The degree of stereoselectivity was relatively low for the agonists isoprenaline and noradrenaline but higher for antagonists and, in particular, tertatolol and propranolol. In mouse ileum, stereoselectivity of propranolol and tertatolol was observed under beta(1)-/beta(2)-adrenoceptor blockade. The (-)-enantiomers of propranolol and tertatolol were more effective at antagonism of (-)-isoprenaline-mediated relaxation of mouse ileum than their (+)-enantiomers. The recombinant mouse, rat and human beta(3)-adrenoceptors display stereoselective interactions for agonists and antagonists similar to the stereoselective profile of beta(3)-adrenoceptors in mouse ileum. The degree of stereoselectivity varied between species and the human beta(3)-adrenoceptor displayed higher affinities and enantiomeric ratios than the mouse or rat beta(3)-adrenoceptors.
Related Concept Videos
Adrenergic Receptors: β Subtype
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors have equal affinities for...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Adrenergic Receptors: ɑ Subtype
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase C—inositol-1,4,5-trisphosphate...
Adrenergic Antagonists: Chemistry and Classification of β-Receptor Blockers
Drug-Receptor Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.

