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Ro60-0213

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Title: Ro60-0213  
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Subject: RS-56812, MPPF, BRL-54443, 6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide, NBUMP
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Ro60-0213

Ro60-0213
Systematic (IUPAC) name
(S)-1-(7-methoxyindeno[1,2-b]pyrrol-1(4H)-yl)propan-2-amine
Clinical data
Legal status
?
Identifiers
ATC code ?
Chemical data
Formula C15H20N2O 
Mol. mass 244.331 g/mol
 YesY   

Ro60-0213 (Org 35032) is a drug developed by Hoffmann–La Roche, which acts as a potent and selective agonist for the 5-HT2C serotonin receptor, with more than 100x selectivity over other closely related serotonin receptor subtypes, and little or no affinity at other receptors. It was developed as a potential antidepressant,[1] but was discontinued from clinical development at an early stage due to toxicity concerns.[2] However the high selectivity of Ro60-0213 for 5-HT2C makes it of continued interest for research into serotonin receptors.[3]

See also

References

  1. ^ Leysen, D.; Kelder, J. (1998). "Ligands for the 5-HT2C receptor as potential antidepressants and anxiolytics" 29. pp. 49–61.  
  2. ^ "Suppression of mutagenic activity of a series of 5HT2c receptor agonists by the incorporation of a gem-dimethyl group: SAR using the Ames test and a DNA unwinding assay". Mutagenesis 13 (4): 397–403. July 1998.  
  3. ^ Shimada, I; Maeno, K; Kazuta, K; Kubota, H; Kimizuka, T; Kimura, Y; Hatanaka, K; Naitou, Y et al. (2008). "Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo2,3-gindazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists". Bioorganic & Medicinal Chemistry 16 (4): 1966–82.  


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