887258-95-9
Chemical Structure
Vabicaserin
Synonym(s): SCA-136 free base
- CAS No.: 887258-95-9
- Formula:C15H20N2
- Molecular Weight:228.33
IUPAC Name: (9aR,12aS)-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline
InChIKey: NPTIPEQJIDTVKR-STQMWFEESA-N
SMILES: [H][C@]1(CCC2)[C@]2([H])CN3C(C1=CC=C4)=C4CNCC3
Biological Activity: 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)[1][2][3][4][5][6][7][8].
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Vabicaserin | 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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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.
