Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
Article Details
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Krogsgaard-Larsen N, Jensen AA, Kehler J
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5431-3. doi: 10.1016/j.bmcl.2010.07.105. Epub 2010 Aug 3.
- PubMed ID
- 20719507 [ View in PubMed]
- Abstract
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles are synthesized using a six-step protocol. Notably, the synthesis route make use of a new and improved ring-closing methodology for the assembly of the hexahydro-pyrazino[1,2-a]indole scaffold, which is based on intramolecular C-H insertion of a carbene. The compounds act as dual serotonin 5-HT2C- and 5-HT6-ligands.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Aripiprazole 5-hydroxytryptamine receptor 2C Ki (nM) 22 N/A N/A Details Aripiprazole 5-hydroxytryptamine receptor 6 Ki (nM) 574 N/A N/A Details Clozapine 5-hydroxytryptamine receptor 2C Ki (nM) 15 N/A N/A Details Clozapine 5-hydroxytryptamine receptor 6 Ki (nM) 17 N/A N/A Details Olanzapine 5-hydroxytryptamine receptor 2C Ki (nM) 14 N/A N/A Details Olanzapine 5-hydroxytryptamine receptor 6 Ki (nM) 6 N/A N/A Details Sertindole 5-hydroxytryptamine receptor 2C Ki (nM) 1 N/A N/A Details Sertindole 5-hydroxytryptamine receptor 6 Ki (nM) 5 N/A N/A Details Ziprasidone 5-hydroxytryptamine receptor 2C Ki (nM) 13 N/A N/A Details Ziprasidone 5-hydroxytryptamine receptor 6 Ki (nM) 61 N/A N/A Details