BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone ( HY-B1115A ) and is metabolized by CYP3A4 .4 . BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe ( EC 50 s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors ( IC 50 s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
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