108061-47-8Relevant articles and documents
Binding of β-carbolines at 5-HT2 serotonin receptors
Grella, Brian,Teitler, Milt,Smith, Carol,Herrick-Davis, Katharine,Glennon
, p. 4421 - 4425 (2003)
A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-β-carbolines was examined at 5-HT2A and 5-HT2C serotonin receptors. Whereas most of the methoxy-substituted derivatives typically displayed affinities similar to their unsubstituted parents, certain (particularly 8-substituted) bromo derivatives displayed enhanced affinity. A binding profile was obtained for selected β-carbolines.
Tetrahydrocarboline analogs as MCH-1 antagonists
Henderson, Alan J.,Deering, Dustin,Grabowski, James F.,Hadden, Mark,Jiang, Xiaowu,Khmelnitsky, Yuri,Luche, Michele,Surman, Matthew D.,Cheetham, Sharon,Vickers, Steven,Viggers, Jean,Guzzo, Peter R.
scheme or table, p. 7024 - 7028 (2011/01/05)
A new series of tetrahydrocarbolines with potent MCH-1 antagonist activity were synthesized, using a conformationally constrained design approach towards optimizing pharmacokinetic properties. Two compounds from this series were progressed to a 5-day diet-induced obesity mouse screening model to evaluate their potential as weight loss agents. Both compounds produced a highly significant reduction in weight, which was attributed to their improved pharmacokinetic profile.