Inhibition of [3H]nicotinic acid binding to rat spleen membranes
| Inhibitor | Ki |
|---|---|
| nM | |
| Nicotinic acid | 33.0 (31.5–34.6) |
| Pyridazine-4-carboxylic acid | 121 (81.7–179) |
| Acipimox | 309 (263–362) |
| 3-Pyridine-acetic acid | 403 (370–439) |
| 5-Methylpyrazine-2-carboxylic acid | 652 (594–716) |
| 5-Methylnicotinic acid | 717 (456–1130) |
| Pyrazine-2-carboxylic acid | 762 (618–940) |
| 6-Methylnicotinic acid | 1700 (1370–2120) |
| Nicotinic acid-1-oxide | 3160 (2810–3550) |
Inhibition of [3H]nicotinic acid (20 nM) binding to rat spleen membranes by nicotinic acid and structurally related compounds was assessed in the presence of 100 μg of membrane protein after 3.5 h of incubation at 25°C, as described underExperimental Procedures. K i values were determined by nonlinear curve fitting and are given as geometric means with 95% confidence limits from at least three independent experiments.