Ro60-0213

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Ro60-0213
Ro60-0213 structure.png
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 (what is this?)  (verify)

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[edit]

References[edit]

  1. ^ Leysen, D.; Kelder, J. (1998). Ligands for the 5-HT2C receptor as potential antidepressants and anxiolytics 29. pp. 49–61. doi:10.1016/S0165-7208(98)80044-5.  edit
  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. doi:10.1093/mutage/13.4.397. PMID 9717178. 
  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. doi:10.1016/j.bmc.2007.10.100. PMID 18035544.