Related Experiment Video
Updated: Aug 8, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
Partial to complete antagonism by putative antagonists at the wild-type alpha(2C)-adrenoceptor based on kinetic
1Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cédex - France. peter.pauwels@pierre-fabre.com
Abstract:
1. Activation of the recombinant human alpha(2C)-adrenoceptor (alpha(2C) AR) by (-)-adrenaline in CHO-K1 cells transiently co-expressing a chimeric G(alpha q/i1) protein induced a rapid, transient Ca(2+) response with a high-magnitude followed by a low-magnitude phase which continued throughout the recorded time period (15 min). 2. Activation of the alpha(2C) AR by various alpha(2) AR agonists revealed the following rank order of high-magnitude Ca(2+) response [E(max) (%) versus 10 microM (-)-adrenaline]: UK 14304 (102+/-4)=talipexole (101+/-3)=(-)-adrenaline (100)=d-medetomidine (98+/-1)>oxymetazoline (81+/-4) reverse similarclonidine (75+/-5). 3. The methoxy- (RX 821002) and ethoxy-derivatives (RX 811059) of idazoxan and the dexefaroxan analogue atipamezole were fully effective as antagonists of both the high- and the low-magnitude Ca(2+) response. However, though acting as full antagonists of the high-magnitude response, the further putative alpha(2) AR antagonists idazoxan (27%), SKF 86466 (29%) and dexefaroxan (59%) reversed the low-magnitude response only partially. 4. In conclusion, kinetic analyses of agonist : antagonist interactions at the alpha(2C) AR demonstrate a wide spectrum of partial to complete antagonism of the low-magnitude Ca(2+) response for structurally related alpha(2) AR ligands.
More Related Videos
09:05Measurement of Smooth Muscle Function in the Isolated Tissue Bath-applications to Pharmacology Research
Published on: January 19, 2015
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Related Concept Videos
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.
Drug-Receptor Interaction: Antagonist
Antagonists can be classified as competitive or noncompetitive based on their...
Combined Effects of Drugs: Antagonism
The most common type is receptor antagonism, where one drug acts as an antagonist to block the effects of another drug by...
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 Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally, α1-blockers effectively address urinary obstruction...