S Röver,
D R Adams, A Bénardeau,
J M Bentley,
M J Bickerdike,
A Bourson,
I A Cliffe,
P Coassolo,
J E P Davidson,
C T Dourish, [......],
A R Knight,
C S Malcolm,
P Mattei,
A Misra,
J Mizrahi,
M Muller,
R H P Porter,
H Richter,
S Taylor,
S P Vickers
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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.
Bioorganic & Medicinal Chemistry Letters 09/2005; 15(15):3604-8. · 2.55 Impact Factor
