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Cat. No.: HY-111200A

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Vabicaserin

Name: Vabicaserin
Brand: MedChemExpress
SKU: HY-111200A
Availability: PreOrder

(Synonyms: SCA-136 free base)

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

Vabicaserin (SCA-136 free base) is a brain-penetrant, orally active, and selective 5-HT_2C receptor agonist (K_i = 3 nM; EC₅₀ = 8 nM). Vabicaserin specifically activates Gq-coupled 5-HT_2C 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-HT_2A/5-HT_2B receptors. Vabicaserin can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).

For research use only. We do not sell to patients.

CAS No.: 887258-95-9
Formula: C₁₅H₂₀N₂
Molecular Weight:228.33

Storage:

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

Vabicaserin Chemical Structure

CAS No.: 887258-95-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Purity & Documentation
References
Calculators
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Classifications
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Biological Activity

Description

IC₅₀ & Target

^[6]

Human 5-HT_2C Receptor

3 nM (Ki)

human 5-HT_2B Receptor

14 nM (Ki)

human 5-HT_1A Receptor

112 nM (Ki)

5-HT_2C Receptor

8 nM (EC₅₀)

5-HT_2A Receptor

1650 nM (EC₅₀)

5-HT_2B Receptor

29 nM (EC₅₀)

All 5-HT Receptor Isoforms :

In Vitro

Vabicaserin (SCA-136 free base) binds to the human 5-HT_2C receptor with high affinity (K_i = 3 nM) and exhibits greater than 50-fold selectivity over other monoamine receptors, with affinity for the 5-HT_2B (K_i = 14 nM) and 5-HT_1A (K_i = 112 nM) receptors^[6].
Vabicaserin is a potent and full 5-HT_2C receptor agonist (EC₅₀ = 8 nM) in CHO cells and acts as an antagonist at 5-HT_2A (IC₅₀ = 1650 nM) and 5-HT_2B (IC₅₀ = 29 nM) receptors, with its 5-HT_2B agonist activity depending on receptor expression levels^[6].
Vabicaserin (30 min) promotes the accumulation of 5-HT_2C-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 (SCA-136 free base) (0.3-3 mg/kg; s.c.; single dose; 30-240 min) restores muscle pressure thresholds and attenuates hyperalgesia in the Reserpine (HY-N0480)-induced myalgia (RIM) rat model^[8].
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.

Animal Model:

Sprague-Dawley rat (male; 250-300g) subcutaneously injected of 1 mg/kg Reserpine once daily for 3 consecutive days^[8]
Dosage:

0.3, 1, 3 mg/kg
Administration:

s.c.; single dose; 30, 60, 120, 240 min
Result:

Recovered the muscle pressure threshold at doses of 1 and 3 mg/kg.
Alleviated myalgia without producing a significant reduction in locomotor activity.

Related Protocols :

Research Protocol for Metabolic Diseases

Chemical Information

CAS No. 887258-95-9
Molecular Weight 228.33
Formula C₁₅H₂₀N₂
SMILES

[H][C@]1(CCC2)[C@]2([H])CN3C(C1=CC=C4)=C4CNCC3
Synonyms

SCA-136 free base
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (5)

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ACS Chem Neurosci

Serotonin 5-HT2C Receptor Signaling Analysis Reveals Psychedelic Biased Agonism. [Abstract]

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
The Medical College of Wisconsin

2026.
Authorea

September 19, 2022.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

[2]. Neelamegam R, et al. Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization. Journal of medicinal chemistry. 2014 Feb 27;57(4):1488-94.

[3]. Ding N, et al. The enhancing effect of 5-HT on phasic contractions of human isolated distal ureter and the mechanisms mediating these effects. European journal of pharmacology. 2023 Jun 15;949:175715.

[4]. Shen JH, et al. A 6-week randomized, double-blind, placebo-controlled, comparator referenced trial of vabicaserin in acute schizophrenia. J Psychiatr Res. 2014 Jun;53:14-22.

[5]. Teixeira-Castro A, et al. Serotonergic signalling suppresses ataxin 3 aggregation and neurotoxicity in animal models of Machado-Joseph disease. Brain : a journal of neurology. 2015 Nov;138(Pt 11):3221-37.

[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]

[7]. Rosenzweig-Lipson, et al. 5-HT₂C Agonists as Therapeutics for the Treatment of Schizophrenia. Novel Antischizophrenia Treatments, edited by M. A. Geyer and G. Gross, vol. 213, Springer, 2012, pp. 147–165.

[8]. Ogino S, et al. Systemic administration of 5-HT(2C) receptor agonists attenuates muscular hyperalgesia in reserpine-induced myalgia model. Pharmacol Biochem Behav. 2013 Jul;108:8-15.

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Purity & Documentation
References

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Vabicaserin

Publications Citing Use of MedChemExpress (MCE) Vabicaserin

All 5-HT Receptor Isoforms