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6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,520 | 4-6 weeks | 4-6 weeks | |
| 50 mg | $1,980 | 4-6 weeks | 4-6 weeks | |
| 100 mg | $2,500 | 4-6 weeks | 4-6 weeks |
| Description | 6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4. This compound exhibits affinity for the serotonin (5-HT) receptor subtype 5-HT1A, demonstrating efficacy in the rat hippocampus and dorsal raphe with half-maximal effective concentrations (EC50s) of 4 and 1 µM, respectively. Furthermore, 6-Hydroxy Buspirone acts as a potent antagonist against dopamine D2, D3, and D4 receptors with half-maximal inhibitory concentrations (IC50s) of 3.1, 4.9, and 0.85 µM, respectively, and inhibits the organic cation transporters 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing human transporters, showcasing a concentration-dependent mechanism. |
| Targets&IC50 | D2 Receptor:3.1 μM, D3 receptor:4.9 μM, 5-HT1A receptor (rat):1 μM (EC50), 5-HT1A receptor (rat):4 μM (EC50), D4 Receptor:0.85 μM |
| Synonyms | BMY 28674, BMS-52821 |
| Molecular Weight | 401.50 |
| Formula | C21H31N5O3 |
| Cas No. | 125481-61-0 |
| Smiles | OC(C(N1CCCCN2CCN(CC2)C3=NC=CC=N3)=O)C4(CC1=O)CCCC4 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Methanol: Soluble Ethanol: Soluble DMSO: Soluble |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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