Pharmacology
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. It has much lower affinity (pKi < 5) for the muscarinic acetylcholine receptors. Asenapine behaves as a partial agonist at the 5-HT1A receptors. At all other targets Asenapine is an antagonist. As of November 2010 Asenapine is also in clinical trials at UC Irvine to treat stuttering.
| Receptor | Affinity (pKi) | Affinity (Ki (nM)) |
|---|---|---|
| 5-HT1A | 8.6 | 2.5 |
| 5-HT1B | 8.4 | 4.0 |
| 5-HT2A | 10.2 | 0.06 |
| 5-HT2B | 9.8 | 0.16 |
| 5-HT2C | 10.5 | 0.03 |
| 5-HT5A | 8.8 | 1.6 |
| 5-HT6 | 9.5 | 0.25 |
| 5-HT7 | 9.9 | 0.13 |
| α1-Adrenergic | 8.9 | 1.2 |
| α2A-Adrenergic | 8.9 | 1.2 |
| α2B-Adrenergic | 9.5 | ? (~0.25) |
| α2C-Adrenergic | 8.9 | 1.2 |
| D1 | 8.9 | 1.4 |
| D2 | 8.9 | 1.3 |
| D3 | 9.4 | 0.42 |
| D4 | 9.0 | 1.1 |
| H1 | 9.0 | 1.0 |
| H2 | 8.2 | 6.2 |
| mACh | < 5 | 8,128 |
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