Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
Article Details
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Heffernan GD, Coghlan RD, Manas ES, McDevitt RE, Li Y, Mahaney PE, Robichaud AJ, Huselton C, Alfinito P, Bray JA, Cosmi SA, Johnston GH, Kenney T, Koury E, Winneker RC, Deecher DC, Trybulski EJ
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
Bioorg Med Chem. 2009 Nov 15;17(22):7802-15. doi: 10.1016/j.bmc.2009.09.023. Epub 2009 Sep 18.
- PubMed ID
- 19836247 [ View in PubMed]
- Abstract
The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT(2A) receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel series of compounds is also presented.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Desipramine Sodium-dependent noradrenaline transporter Ki (nM) 0.6 7.4 37 Details Maprotiline Sodium-dependent noradrenaline transporter Ki (nM) 12 7.4 37 Details Mianserin 5-hydroxytryptamine receptor 2A Ki (nM) 3 7.4 22 Details Olanzapine 5-hydroxytryptamine receptor 2A Ki (nM) 4 7.4 22 Details Reboxetine Sodium-dependent noradrenaline transporter Ki (nM) 0.3 7.4 37 Details