Table 1. Effects of Clotrimazole, Itraconazole, Quercetin, and TIPT on the β-Arrestin Recruitment Assay for CCR4, CX3CR1, and V2Ra.
| GPCR | CCR4 | CX3CR1 | V2R | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Compound | Centrifugation | Detergent | Centrifugation | Detergent | Centrifugation | Detergent | |||
| pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | pIC50 ± SEM (IC50 (μM)) | |
| Clotrimazole | NEb | NEb | NEb | 5.7 ± 0.3 (2.0) | 5.0 ± 0.1(10.8 μM) | 5.1 ± 0.7 (7.9) | 5.6 ± 0.1 (2.7) | 4.8 ± 0.2 (15.1) | NEb |
| Itraconazole | 6.3 ± 0.2 (0.5) | 5.1 ± 0.1(7.2 μM) | 4.9 ± 0.4 (11.4) | 6.8 ± 0.2 (0.1) | 5.3 ± 0.2(5.0 μM) | 4.7 ± 0.3 (20.8) | 6.1 ± 0.2 (0.8) | 4.9 ± 0.1 (11.9) | 5.2 ± 0.2 (6.0) |
| Quercetin | 5.0 ± 0.3 (10.2) | <4.5 (>100 μM) | <4.5 (>100) | 5.3 ± 0.3 (4.5) | NEb | <4 (>32) | 5.2 ± 0.1 (7.0) | 4.4 ± 0.3 (37.8) | 4.8 ± 0.3 (15.2) |
| TIPT | 5.4 ± 0.3 (3.5) | NEb | 5.0 ± 0.4 (9.9) | 5.7 ± 0.3 (2.2) | NEb | <4 (>32) | 6.4 ± 0.1 (0.4) | NEb | 4.3 ± 0.3 (45.0) |
a
. The pIC50 and corresponding IC50 values on direct treatment with aggregators, after centrifugation, and with detergent are shown.
b
No effect on receptor activity.