An active metabolite of buspirone
Related Products
Isomer(s)
342075-hydroxy Buspirone
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6-hydroxy Buspirone

Item No. 39807

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-hydroxy-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
CAS Number
125481-61-0
Synonyms
  • BMS-52821
  • BMY 28674
Molecular Formula
C21H31N5O3
Formula Weight
401.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
OC(C(N1CCCCN2CCN(CC2)C3=NC=CC=N3)=O)C4(CC1=O)CCCC4
InChi Code
InChI=1S/C21H31N5O3/c27-17-16-21(6-1-2-7-21)18(28)19(29)26(17)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20/h5,8-9,18,28H,1-4,6-7,10-16H2
InChi Key
KOZNAHJIJGCFJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $258

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    5 mg

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    Product Description

    6-hydroxy Buspirone is an active metabolite of the anxiolytic buspirone.1,2,3 It is formed from buspirone by the cytochrome P450 (CYP) isoform CYP3A4.4 6-hydroxy Buspirone binds to the serotonin (5-HT) receptor subtype 5-HT1A in rat hippocampus and dorsal raphe (EC50s = 4 and 1 µM, respectively) and is a dopamine D2, D3, and D4 receptor antagonist (IC50s = 3.1, 4.9, and 0.85 µM, respectively).1,2 It also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 in S2 proximal tubule cells expressing the human transporters in a concentration-dependent manner.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wong, H., Dockens, R.C., Pajor, L., et al. 6-Hydroxybuspirone is a major active metabolite of buspirone: Assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metab. Dispos. 35(8), 1387-1392 (2007).

    2. Bergman, J., Roof, R.A., Furman, C.A., et al. Modification of cocaine self-administration by buspirone (Buspar®): Potential involvement of D3 and D4 dopamine receptors. Int. J. Neuropsychopharmacol. 16(2), 445-458 (2013).

    3. Jinakote, M., Jutabha, P., Anzai, N., et al. Interaction of buspirone and its major metabolites with human organic cation transporters. Fundam. Clin. Pharmacol. 37(4), 833-842 (2023).

    4. Zhu, M., Zhao, W., Jimenez, H., et al. Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Drug Metab. Dispos. 33(4), 500-507 (2005).