BMY 28674 (Synonyms: 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215)

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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.

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BMY 28674 Chemical Structure

CAS No. : 125481-61-0

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Other Forms of BMY 28674:

BMY 28674-d₈ Get quote

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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Purity & Documentation
References
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Description

IC₅₀ & Target

Rat 5-HT_1A Receptor

4 μM (EC₅₀)

D₂ Receptor

3.1 μM (IC₅₀)

D₃ Receptor

4.9 μM (IC₅₀)

D₄ Receptor

0.85 μM (IC₅₀)

Rat 5-HT_1A Receptor

1 μM (EC₅₀)

Molecular Weight

401.50

Formula

C₂₁H₃₁N₅O₃

CAS No.

125481-61-0

SMILES

O=C(N(CCCCN1CCN(C2=NC=CC=N2)CC1)C(C3)=O)C(O)C43CCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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 Related Classifications

Neurological Disease

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMY 28674125481-61-06-Hydroxybuspirone 6'-Hydroxybuspirone BMS 528215BMY28674BMY-28674BMS528215BMS 528215BMS-5282155-HT ReceptorDopamine ReceptorOthersSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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