Vabicaserin
Based on 5 publication(s) in Google Scholar
Vabicaserin (SCA-136 free base) is a brain-penetrant, orally active, and selective 5-HT2C receptor agonist (Ki = 3 nM; EC50 = 8 nM). Vabicaserin specifically activates Gq-coupled 5-HT2C receptors to promote calcium mobilization, thereby selectively reducing dopamine release in the mesolimbic system without affecting the nigrostriatal pathway. Vabicaserin is an antagonist of 5-HT2A/5-HT2B receptors. Vabicaserin can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).
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- No. CAS: 887258-95-9
- Fòrmula: C15H20N2
- Peso molecular:228.33
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Vabicaserin
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Actividad biológica
Descripciòn
IC50 & Target
[6]|
Human 5-HT2C Receptor 3 nM (Ki) |
human 5-HT2B Receptor 14 nM (Ki) |
human 5-HT1A Receptor 112 nM (Ki) |
5-HT2C Receptor 8 nM (EC50) |
5-HT2A Receptor 1650 nM (EC50) |
5-HT2B Receptor 29 nM (EC50) |
In Vitro
Vabicaserin is a potent and full 5-HT2C receptor agonist (EC50 = 8 nM) in CHO cells and acts as an antagonist at 5-HT2A (IC50 = 1650 nM) and 5-HT2B (IC50 = 29 nM) receptors, with its 5-HT2B agonist activity depending on receptor expression levels[6].
Vabicaserin (30 min) promotes the accumulation of 5-HT2C-coupled inositol monophosphate (IP1) in CHO cells with an EC50 of 32 nM[6].
Vabicaserin exhibits activity in increasing the frequency of spontaneous or NKA (HY-P0197)-induced rhythmic contractions in human distal ureteral tissue cell strips[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vabicaserin ameliorates mutant ATXN3-mediated motor dysfunction in the C. elegans AT3q130 model[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rat (male; 250-300g) subcutaneously injected of 1 mg/kg Reserpine once daily for 3 consecutive days[8]
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Dosage:0.3, 1, 3 mg/kg
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Administration:s.c.; single dose; 30, 60, 120, 240 min
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Result:Recovered the muscle pressure threshold at doses of 1 and 3 mg/kg.
Alleviated myalgia without producing a significant reduction in locomotor activity.
Chemical Information
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No. CAS 887258-95-9
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Peso molecular 228.33
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Fòrmula C15H20N2
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SMILES
[H][C@]1(CCC2)[C@]2([H])CN3C(C1=CC=C4)=C4CNCC3
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Synonyms
SCA-136 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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ACS Chem Neurosci
2025 Oct 1;16(19):3899-3914. PMID: 40944639 -
Neuroscience
Selective Serotonin Reuptake Inhibitors and 5-HT2 Receptor Agonists Have Distinct, Sleep-state Dependent Effects on Postictal Breathing in Amygdala Kindled Mice. [Abstract]2023 Mar 1:513:76-95. PMID: 36702372 -
Epilepsy Behav
MK-212 precipitates seizure-induced death in amygdala-kindled mice via a non-5-HT2C receptor-mediated mechanism. [Abstract]2025 Jun:167:110385. PMID: 40132446 -
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Pureza y Documentación
Referencias
[1]. Chen W. Repeated administration of 5‐hydroxytryptamine 2C agonist MK212 produces a sensitization effect of antipsychotic activity. IUBMB life. 2016 Dec;68(12):985-93. [Content Brief]
[6]. Dunlop J, et al. Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. The Journal of pharmacology and experimental therapeutics. 2011 Jun;337(3):673-80. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Vabicaserin Related Classifications
HY-111200A Related Classifications
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