126062-51-9Relevant articles and documents
N-methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT(1D) receptor agonist
Xu, Yao-Chang,Schaus, John M.,Walker, Clint,Krushinski, Joe,Adham, Nika,Zgombick, John M.,Liang, Sidney X.,Kohlman, Dan T.,Audia, James E.
, p. 526 - 531 (2007/10/03)
It has been observed that reported 5-HT(1D) receptor agonists have at least one heteroatom (N, O, or S) on the 5-substituent of the indole. This has led to the hypothesis that a 5-substituent capable of participating in hydrogen bonding is critical for conveying high affinity. This article describes the synthesis and biological evaluation of a new series of 5- alkyltryptamine analogues, which does not have a heteroatom in the 5- substituent group. In contrast to the hypothesis, 5-alkyltryptamines all exhibit high binding affinities for the human 5-HT(1D) receptor. The size of the lipophilic alkyl group at the 5-position of the indole has significant impact on the 5-HT(1D) binding affinity. Compounds with a tert-butyl group at the 5-position such as 9d, 10, and 11 were identified. These analogues display high binding affinity (K(i) 1 nM) and moderate receptor selectivity in comparison with known antimigraine agents such as sumatriptan, naratriptan, rizatriptan, and VML-251.
METHOD FOR TREATING 5HT2B RECEPTOR RELATED CONDITIONS
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, (2008/06/13)
The present invention provides methods for binding a 5-HT 2B receptor in mammals using a both known and novel compounds. Further, the invention provides a method for treating or preventing 5-HT 2B related conditions. Finally, the invention provides an article of manufacture.
Tetrahydro-β-carbolines
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, (2008/06/13)
The present invention provides tetrahydro-betacarboline compounds having useful central nervous system activity.