GPCR assays

Adrenoceptor Assays

Species: Human

Subtypes: α1A, α1B, α2A, α2C, β1, β2 (others available on request)

Assay Formats: Radioligand binding (α1A, α1B, α2A, α2C), Cell-based assay (α1A, α2A, β1, β2)

Services: HTS, single concentration / dose response studies, selectivity profiling

 

Adrenoceptor α1A - Ligand binding assay

Adrenoceptor a1A binding assay

Figure 1: Dose response curve for Clozapine in an Adrenergic α1A radioligand binding assay. Approximate IC50 42nM.

 

Adrenoceptor α1B - Ligand binding assay

Adrenoceptor a1B binding assay

Figure 2: Dose response curve for Clozapine in an Adrenergic α1B radioligand binding assay. Approximate IC50 28μM.

 

Adrenoceptor α2A - Ligand binding assay

Adrenoceptor a2A binding assay

Figure 3: Dose response curve for Clozapine in an Adrenergic α2A radioligand binding assay. Approximate IC50 2.8μM.

 

Adrenoceptor α2C - Ligand binding assay

Adrenoceptor a2C binding assay

Figure 4: Dose response curve for Clozapine in an Adrenergic α2C radioligand binding assay. Approximate IC50 2.8μM.

 

Adrenoceptor α1A - Cell-based assay

Adrenoceptor a1A cell based assay

Figure 5: Dose response curve for agonist R-Phenylephrine in an Adrenergic α1A cell-based assay. Approximate EC50 32.8 nM.

 

Adrenoceptor α1A - Cell-based assay

Adrenoceptor a1A cell based assay

Figure 6: Dose response curve for antagonist Carvedilol in an Adrenergic α1A cell-based assay. Approximate IC50 60 nM.

 

Adrenoceptor α2A - Cell-based assay

Adrenoceptor a2A cell based assay

Figure 7: Dose response curve for agonist Phenylephrine hydrochloride in an Adrenergic α2A cell-based assay. Approximate EC50 697 nM.

 

Adrenoceptor α2A - Cell-based assay

Adrenoceptor a1A cell based assay

Figure 8: Dose response curve for antagonist BRL 44408 in an Adrenergic α2A cell-based assay. Approximate IC50 1.38 nM.

 

Adrenoceptor β1 - Cell-based assay

Adrenoceptor B1 cell based assay

Figure 9: Dose response curve for agonist Isoprenaline in an Adrenergic β1 cell-based assay. Approximate EC50 14 nM.

 

Adrenoceptor β1 - Cell-based assay

Adrenoceptor B1 cell based assay

Figure 10: Dose response curve for antagonist Carvedilol in an Adrenergic β1 cell-based assay. Approximate IC50 35 nM.

 

Adrenoceptor β2 - Cell-based assay

Adrenoceptor B2 cell based assay

Figure 11: Dose response curve for agonist Isoprenaline in an Adrenergic β2 cell-based assay. Approximate EC50 26 nM.

 

Adrenoceptor β2 - Cell-based assay

Adrenoceptor B2 cell based assay

Figure 12: Dose response curve for antagonist Carvedilol in an Adrenergic β2 cell-based assay. Approximate IC50 2 nM.


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