C6H6
Bluelighter
- Joined
- Jan 29, 2005
- Messages
- 607
Anyone with access to this journal care to get this article and post it here? Sounds interesting, there are probably also affinity data for other, more interesting receptors.
Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Slassi A, Edwards L, O'Brien A, Meng CQ, Xin T, Seto C, Lee DK, MacLean N, Hynd D, Chen C, Wang H, Kamboj R, Rakhit S.
NPS Allelix Corp., Mississauga, Ontario, Canada. [email protected]
A series of 5-alkyltryptamines (6) and the corresponding conformationally constrained analogues (8) have been synthesized. The structure activity relationships (SAR) at the 5-position of the indole skeleton and the ethylamine side chain have been studied. Functional activities were assessed using isolated rabbit saphenous vein. Potent, selective ligands were found (6e, Ki 2.5 nM, 5-HT1B/5-HT1D 125-fold) that have potential for treating acute migraine.
PMID: 10937729
Bioorg Med Chem Lett. 2000 Aug 7;10(15):1707-9.
5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists.
Slassi A, Edwards L, O'Brien A, Meng CQ, Xin T, Seto C, Lee DK, MacLean N, Hynd D, Chen C, Wang H, Kamboj R, Rakhit S.
NPS Allelix Corp., Mississauga, Ontario, Canada. [email protected]
A series of 5-alkyltryptamines (6) and the corresponding conformationally constrained analogues (8) have been synthesized. The structure activity relationships (SAR) at the 5-position of the indole skeleton and the ethylamine side chain have been studied. Functional activities were assessed using isolated rabbit saphenous vein. Potent, selective ligands were found (6e, Ki 2.5 nM, 5-HT1B/5-HT1D 125-fold) that have potential for treating acute migraine.
PMID: 10937729
