Ro60-0213

{{Short description|Chemical compound}}

{{Drugbox

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| verifiedrevid = 433025850

| IUPAC_name = (S)-1-(7-methoxyindeno[1,2-b]pyrrol-1(4H)-yl)propan-2-amine

| image = Ro60-0213.svg

| width = 240

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| CAS_number = 170493-66-0

| ChEMBL = 2114265

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| PubChem = 3045239

| ChemSpiderID = 2308013

| C=15 | H=18 | N=2 | O=1

| smiles = C[C@@H](Cn1ccc2c1-c3cc(ccc3C2)OC)N

| StdInChI = 1S/C15H18N2O/c1-10(16)9-17-6-5-12-7-11-3-4-13(18-2)8-14(11)15(12)17/h3-6,8,10H,7,9,16H2,1-2H3/t10-/m0/s1

| StdInChIKey = OTCPUISFVUWAGR-JTQLQIEISA-N

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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,{{Cite book | vauthors = Leysen D, Kelder J | doi = 10.1016/S0165-7208(98)80044-5 | chapter = Ligands for the 5-HT2C receptor as potential antidepressants and anxiolytics | volume = 29 | pages = 49–61 | year = 1998 | title = Trends in Drug Research II, Proceedings of the 11th Noordwijkerhout-Camerino Symposium | series = Pharmacochemistry Library | isbn = 9780444826336 }} but was discontinued from clinical development at an early stage due to toxicity concerns.{{cite journal | vauthors = Albertini S, Bös M, Gocke E, Kirchner S, Muster W, Wichmann J | title = 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 | journal = Mutagenesis | volume = 13 | issue = 4 | pages = 397–403 | date = July 1998 | pmid = 9717178 | doi = 10.1093/mutage/13.4.397 | doi-access = free }} However the high selectivity of Ro60-0213 for 5-HT2C makes it of continued interest for research into serotonin receptors.{{cite journal | vauthors = Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S | display-authors = 6 | title = Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 4 | pages = 1966–82 | date = February 2008 | pmid = 18035544 | doi = 10.1016/j.bmc.2007.10.100 }}

See also

References