GPCR assays

Serotonin (5HT) Receptor Assays

Species: Human

Subtypes: 5HT1A, 5HT1B, 5HT2A, 5HT2B, 5HT2C, 5HT6, 5HT7 (others available on request)

Assay Formats: Radioligand binding (5HT1A, 5HT2A, 5HT2C, 5HT6, 5HT7), Cell-based assay (5HT1A, 5HT1B, 5HT2A, 5HT2B)

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

 

Serotonin 5HT1A - Ligand binding assay

5HT1a binding assay

Figure 1: Dose response curve for Clozapine in a Serotonin 5HT1A radioligand binding assay. Approximate IC50 364nM.

 

Serotonin 5HT2A - Ligand binding assay

5HT2a binding assay

Figure 2: Dose response curve for Clozapine in a Serotonin 5HT1C radioligand binding assay. Approximate IC50 9nM.

 

Serotonin 5HT2C - Ligand binding assay

5HT2c binding assay

Figure 3: Dose response curve for Clozapine in a Serotonin 5HT2C radioligand binding assay. Approximate IC50 28nM.

 

Serotonin 5HT6 - Ligand binding assay

5HT6 binding assay

Figure 4: Dose response curve for Clozapine in a Serotonin 5HT6 radioligand binding assay. Approximate IC50 36nM.

 

Serotonin 5HT7 - Ligand binding assay

5HT7 binding assay

Figure 5: Dose response curve for Clozapine in a Serotonin 5HT7 radioligand binding assay. Approximate IC50 635nM.

 

Serotonin 5HT1A - Cell-based assay

5HT1A cell based assay

Figure 6: Dose response curve for agonist 5HT in a 5HT1A cell-based assay. Approximate EC50 7.7 nM.

 

Serotonin 5HT1A - Cell-based assay

5HT1A cell based assay

Figure 7: Dose response curve for antagonist Yohimbine in a 5HT1A cell-based assay. Approximate IC50 439 nM.

 

Serotonin 5HT1B - Cell-based assay

5HT1B cell based assay

Figure 8: Dose response curve for agonist 5HT in a 5HT1B cell-based assay. Approximate EC50 4.7 nM.

 

Serotonin 5HT1B - Cell-based assay

5HT1B cell based assay

Figure 9: Dose response curve for antagonist Yohimbine in a 5HT1B cell-based assay. Approximate IC50 1.88 μM.

 

Serotonin 5HT2A - Cell-based assay

5HT2A cell based assay

Figure 10: Dose response curve for agonist α-methyl-5HT in a 5HT2A cell-based assay. Approximate EC50 228 nM.

 

Serotonin 5HT2A - Cell-based assay

5HT2A cell based assay

Figure 11: Dose response curve for antagonist Clozapine in a 5HT2A cell-based assay. Approximate IC50 5.5 nM.

 

Serotonin 5HT2B - Cell-based assay

5HT2B cell based assay

Figure 12: Dose response curve for agonist α-methyl-5HT in a 5HT2B cell-based assay. Approximate EC50 1.1 nM.

 

Serotonin 5HT2B - Cell-based assay

5HT2B cell based assay

Figure 13: Dose response curve for antagonist Clozapine in a 5HT2B cell-based assay. Approximate IC50 2.37 μM.


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