BMY 28674 (6-Hydroxybuspirone) is a significant drug metabolite of the anxiolytic agent buspirone, primarily metabolized by CYP3A4. This compound exhibits selective binding to the serotonin receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe, with effective concentrations (EC50s) of 4 μM and 1 μM, respectively. Additionally, BMY 28674 acts as an antagonist at dopamine D2, D3, and D4 receptors, demonstrating inhibitory constants (IC50s) of 3.1 μM, 4.9 μM, and 0.85 μM, respectively. Moreover, it inhibits the activity of organic cation transporters OCT1, OCT2, and OCT3 in human proximal tubule cells in a concentration-dependent manner, making it relevant for pharmacological studies involving these receptors and transporters.
BMY 28674 (6-Hydroxybuspirone) is a significant drug metabolite of the anxiolytic agent buspirone, primarily metabolized by CYP3A4. This compound exhibits selective binding to the serotonin receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe, with effective concentrations (EC50s) of 4 μM and 1 μM, respectively. Additionally, BMY 28674 acts as an antagonist at dopamine D2, D3, and D4 receptors, demonstrating inhibitory constants (IC50s) of 3.1 μM, 4.9 μM, and 0.85 μM, respectively. Moreover, it inhibits the activity of organic cation transporters OCT1, OCT2, and OCT3 in human proximal tubule cells in a concentration-dependent manner, making it relevant for pharmacological studies involving these receptors and transporters.
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