Vabicaserin
Based on 5 publication(s) in Google Scholar
Vabicaserin is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
For research use only. We do not sell to patients.
- CAS No.: 887258-95-9
- Formula: C15H20N2
- Molecular Weight:228.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Vabicaserin
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Biological Activity
Description
IC50 & Target
EC50: 8 nM (5-HT2C Receptor)[1]
In Vitro
Vabicaserin displaces 125I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT2C receptor sites in Chinese hamster ovary cell membranes with a Ki value of 3 nM and is >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors. Binding affinity determined for the human 5-HT2B receptor subtype using [3H]5HT is 14 nM. Vabicaserin is a potent and full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization and exhibits 5-HT2A receptor antagonism and 5-HT2B antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression. Vabicaserin exhibits lower affinity at the 5-HT2C antagonist binding site (22 nM) labeled with [3H]mesulergine. Additional binding studies indicate that Vabicaserin possesses affinity for the 5-HT2B and 5-HT1A receptors with Ki values of 14 and 112 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 887258-95-9
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Molecular Weight 228.33
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Formula 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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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.
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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Protocol
Animal Administration[2]
Mice and Rats[2]
For metabolism studies in mice, rats, and dogs, radiolabeled doses are used. Male and female CD-1 mice and Sprague-Dawley rats are used. The dose vehicle for mice and rats contained 2% (w/w) Tween 80 and 0.5% methylcellulose in water. Nonfasted male and female mice weighing from 27.8 to 33.8 g at the time of dosing are given a single 50-mg/kg (∼300 μCi/kg) dose of Vabicaserin at a volume of 20 mL/kg via intragastric gavage. Mice are kept in metabolic cages in groups of five. Nonfasted male rats weighing from 318 to 345 g and female rats weighing from 227 to 255 g at the time of dosing are given a single 5-mg/kg (∼300 μCi/kg) dose of Vabicaserin at a volume of 2.5 mL/kg via intragastric gavage. Four bile duct-cannulated male rats weighing from 387 to 411 g and four bile duct-cannulated female rats weighing from 291 to 325 g at the time of dosing are nonfasted and are given a single 5-mg/kg (323 μCi/kg) dose of Vabicaserin at a volume of 5.0 mL/kg via intragastric gavage. Rats are kept individually in metabolism cages[2].
Dogs[2]
Four male beagle dogs, weighing from 7.6 to 9.8 kg at the time of dosing, are from an in-house colony. Approximately 11 mg of [14C]Vabicaserin hydrochloride and 940 mg of nonlabeled Vabicaserin hydrochloride are dissolved in methanol and then evaporated under a nitrogen stream to dryness. Capsules (number 2) are filled with accurate amounts (126.7-138.1 mg) of the mixed drug substance according to animal weights to give a dosage of 15 mg/kg (39 μCi/kg). The filled gelatin capsules are then enteric-coated manually. Each dog is given one enteric-coated capsule containing [14C]Vabicaserin as the hydrochloride salt. Animals are fed 2 h before dosing and are housed individually in metabolic cages[2].
Monkey[2]
Four male cynomolgus monkeys, weighing from 5.4 to 9.6 kg at the time of dosing, are from an in-house colony. Nonfasted monkeys are given a single 25-mg/kg dose of nonradiolabeled Vabicaserin at a volume of 2 mL/kg via intragastric gavage. The vehicle is the same as used in mice and rats. Animals are housed individually in metabolic cages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)