Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists |
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| Authors: | Röver S Adams D R Bénardeau A Bentley J M Bickerdike M J Bourson A Cliffe I A Coassolo P Davidson J E P Dourish C T Hebeisen P Kennett G A Knight A R Malcolm C S Mattei P Misra A Mizrahi J Muller M Porter R H P Richter H Taylor S Vickers S P |
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| Affiliation: | Vernalis Research Ltd., Oakdene Court, 613 Reading Road, Wokingham RG41 5UA, UK. stephan.roever@roche.com |
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| Abstract: | Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT(2C) receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT(2) receptor subtypes of 1 order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT(2C) receptor agonists. |
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