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.
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- CAS No.: 42021-34-1
- Formule: C24H26FN3O
- Masse moléculaire:391.48
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Activité biologique
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Chemical Information
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Activité biologique
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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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Masse moléculaire 391.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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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