Percentages of inhibition of specific binding at CGRPR, CB2R, and M3R
| Compound | Displacement of radioligand binding (%) (compounds at 10 µM) | ||
|---|---|---|---|
| hCGRPR | hCB2R | hM3R | |
| 1a | −1.0 ± 4.3 | 7.3 ± 0.3 | −4.1 ± 3.1 |
| 11a | 14.3 ± 1.8 | 32.8 ± 2.8 | –3.9 ± 8.6 |
hCGRPR: human calcitonin gen-related peptide receptor; hCB2R: human cannabinoid receptor, subtype 2; hM3R: human muscarinic receptor, subtype 3. In all cases, data are from two experiments in duplicate. Radioligands used: hCGRPR: [125]hGCRPα, agonist hGCRPα (1 µM); hCB2R: [3H]WIN 55212-2, agonist (5 µM); hM3R: [3H]4-DMAP, agonist 4-DMAP (1 µM)