Biriperone
Biriperone is a D1, D2, and 5-HT2A receptor antagonist with pKi values of 6.372, 7.88 and 7.619. Biriperone blocks amphetamine-induced hyperactivity and stereotypy in rodents. Biriperone blocks secondary conditioned avoidance responses in rodents. Biriperone can be used for the research of schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 42021-34-1
- Formula: C24H26FN3O
- Molecular Weight:391.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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D1 Receptor 6.372 (pKi) |
D2 Receptor 7.88 (pKi) |
5-HT2A Receptor 7.619 (pKi) |
Biriperone (compound 2) binds to D1, D2 and 5-HT2A receptors in rat brain, with pKi values of 6.372, 7.88 and 7.619, respectively, and the pKi ratio of 5-HT2A/D2 is 0.96[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Biriperone (i.p.; single dose) blocks secondary conditioned avoidance response in rats, with an ED50 of 0.04 mg/kg, demonstrating efficacy in suppressing learned avoidance behaviors[1].
Biriperone (i.p.; single dose) blocks unconditioned response in rats, with an ED50 of 9.80 mg/kg, indicating a higher dose requirement for motor reflex suppression compared to conditioned responses[1].
Biriperone (i.p.; single dose) reduces amphetamine-induced hyperactivity in mice, with an ED50 of 0.75 mg/kg, confirming its in vivo D2 receptor blocking activity in the mesolimbic pathway[1].
Biriperone (i.p.; single dose) antagonizes amphetamine-induced toxicity in mice, with an ED50 of 1.00 mg/kg, demonstrating protective effects against dopaminergic overstimulation[1].
Biriperone (i.p.; single dose) induces motor incoordination in mice in the rota rod test, with an ED50 of 2.55 mg/kg, indicating its potential for extrapyramidal side effects at higher doses[1]. Biriperone (i.p.; single dose) induces catalepsy in rats, with an ED50 of 0.86 mg/kg, and a catalepsy/CAR ED50 ratio of 9.5, suggesting a narrower therapeutic window for extrapyramidal side effects compared to compound 5[1]. Biriperone (i.p.; single dose) reduces spontaneous motor activity in rodents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 42021-34-1
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Molecular Weight 391.48
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Formula C24H26FN3O
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SMILES
O=C(C(C=C1)=CC=C1F)CCCN2CC3CC4=C(CN3CC2)NC5=CC=CC=C45
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Synonyms
Centbutindole
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Chakrabarty R, et al. Rational design, synthesis and evaluation of (6aR( *),11bS( *))-1-(4-fluorophenyl)-4-{7-[4-(4-fluorophenyl)-4-oxobutyl]1,2,3,4,6,6a,7,11b,12,12a(RS)-decahydropyrazino[2',1':6,1]pyrido[3,4-b]indol-2-yl}-butan-1-one as a potential neuroleptic agent. Bioorg Med Chem. 2007 Dec 1;15(23):7361-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Biriperone Related Classifications
HY-137935 Related Classifications
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