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Reagent Details

Adrenoceptor family

Catalogue number: CA201261
Product: β3 agonist [(S)-carazolol]
Selectivity: β1: 6.44 | β2: 8.76 | β3: 7.24

 

 
Pharmacophore        (S)-Carazolol-derivative Catalogue Number Pack Size Price
Molecular Weight       933 CA201261-TK0* 0.05 mg £137.50*
Purity ≥97% CA201261-020 0.2 mg £500
Excitation 633 nm CA201261-050 0.5 mg £1200
Emission 650 nm CA201262-100 1.0 mg £2150
 
* Ordered as part of a TestKit comprising a selection of 4 ligands, listing 4 catalogue numbers ending in -TK0
 

Applications

For imaging at β1 / β2 / β3 adrenoceptors use solutions up to 100 nM.

Pharmacological Validation

The CA201261 ligand is a partial agonist at β3 adrenoceptors, is a very weak partial agonist at β1, and has no agonist activity at β2.
 
The CA201261 ligand acts as an antagonist at β1, β2 and β3.
 
The agonist activity of the CA201261 ligand was shown by treating three separate recombinant CHO cell lines expressing either the human β1, β2 or β3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene with the CA201262 ligand at concentrations between 0.1nM and 10µM. The cyclic AMP-induced expression of SPAP was measured under basal, ligand-treated, forskolin-stimulated and 1µM isoprenaline-stimulated conditions. The EC50 value for the CA201262 ligand was calculated from the concentration-response curve. The maximal response achieved with the CA201262 ligand was compared to the maximal response achieved with 1µM isoprenaline, and expressed as a percentage of this maximal response.
 
The antagonist activity of the CA201261 ligand was shown by blocking the activity of the non-selective β agonist, isoprenaline, in the same three CHO cell lines expressing either the human β1, β2 or β3 receptor and the SPAP reporter gene.
 
The cyclic AMP-induced expression of SPAP was measured under basal and forskolin-stimulated (maximal) conditions.  Cells were treated with varying concentrations of isoprenaline alone, or in the presence of 1µM CA201261, and the cyclic AMP-induced expression of SPAP measured.
 
The apparent KD was calculated from the rightward shift of the agonist response curve in the presence of CA201261, compared to the response curve for the agonist alone, for β1, β2 and β3 receptor expressing cell lines.

 



 

 

 

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