| Bioactivity | BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone. It is formed from buspirone via the cytochrome P450 (CYP) isozyme CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). It also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner. |
| CAS | 125481-61-0 |
| Formula | C21H31N5O3 |
| Molar Mass | 401.50 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Zhu, et al. Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab. Dispos. 33(4), 500-507 (2005). |
BMY 28674
CAS: 125481-61-0 F: C21H31N5O3 W: 401.50
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone. It is formed from buspirone via the
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