| 词条 | Ro60-0213 |
| 释义 |
| Watchedfields = changed | verifiedrevid = 433025850 | IUPAC_name = (S)-1-(7-methoxyindeno[1,2-b]pyrrol-1(4H)-yl)propan-2-amine | image = Ro60-0213 structure.png | width = 240 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = 3045239 | ChemSpiderID = 2308013 | C=15 | H=20 | N=2 | O=1 | molecular_weight = 244.331 g/mol | 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 | melting_point = | melting_high = }}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
References1. ^{{Cite journal | last1 = Leysen | first1 = D. | last2 = Kelder | first2 = J. | doi = 10.1016/S0165-7208(98)80044-5 | title = Ligands for the 5-HT2C receptor as potential antidepressants and anxiolytics | volume = 29 | pages = 49–61 | year = 1998 | pmid = | pmc = }} {{Serotonergics}}{{nervous-system-drug-stub}}2. ^{{cite journal | pmid = 9717178 | volume=13 | issue=4 | 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 |date=July 1998 | journal=Mutagenesis | pages=397–403 | doi=10.1093/mutage/13.4.397}} 3. ^{{cite journal | last1 = Shimada | first1 = I | last2 = Maeno | first2 = K | last3 = Kazuta | first3 = K | last4 = Kubota | first4 = H | last5 = Kimizuka | first5 = T | last6 = Kimura | first6 = Y | last7 = Hatanaka | first7 = K | last8 = Naitou | first8 = Y | last9 = Wanibuchi | first9 = F | last10 = Sakamoto | first10 = Shuichi | last11 = Tsukamoto | first11 = S | title = Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo2,3-gindazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 4 | pages = 1966–82 | year = 2008 | pmid = 18035544 | doi = 10.1016/j.bmc.2007.10.100 | display-authors = 8 }} 2 : Serotonin receptor agonists|Hoffmann-La Roche |
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