EC50 and Ki values of nicotinic acid and related compounds
| Compound | Rata | Humanb | ||||
|---|---|---|---|---|---|---|
| GTPγS Binding Assay (EC50) | [3H]Nicotinic Acid Binding Assay (Ki) | GTPγS Binding Assay (EC50) | [3H]Nicotinic Acid Binding Assay (Ki) | |||
| Adipocytes | Spleen | Spleen | HCA2 (Cloned) | HCA2 (Cloned) | Adipocytes | |
| μM | ||||||
| Nicotinic acid | 1.4 | 0.70 | 0.033 | 0.25 | 0.081 | 0.079 |
| Acifran | N.D. | N.D. | N.D. | 2.1 | 1.1 | 0.83 |
| Acipimox | 10 | 6.6 | 0.31 | 6.0 | 5.1 | 4.3 |
| 3-Pyridine-acetic acid | 16 | 17 | 0.40 | 5.5 | 0.54 | 0.55 |
| Pyridazine-4-COOH | 3.8 | 3.1 | 0.12 | N.D. | N.D. | N.D. |
| Pyrazine-2-COOH | 26 | 22 | 0.76 | N.D. | N.D. | N.D. |
| 5-Me-nicotinic acid | 30 | 30 | 0.72 | 8.7 | 4.12 | 3.68 |
| 5-Me-pyrazine-2-COOH | 52 | 15 | 0.65 | N.D. | N.D. | N.D. |
| 6-Me-nicotinic acid | 73 | 54 | 1.7 | N.D. | N.D. | N.D. |
| Nicotinic acid-1-oxide | 80 | 74 | 3.2 | N.D. | N.D. | N.D. |
| 2-OH-nicotinic acid | 132 | N.D. | N.D. | N.D. | N.D. | N.D. |
| Furan-3-COOH | 142 | N.D. | N.D. | N.D. | N.D. | N.D. |
| Nicotinamide | >1000 | >1000 | N.D. | >1000 | 92 | 75 |