5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
A series of 5-(2- or 3-thienyl)tryptamine derivatives (9) has been synthesized and shown to be potent and selective 5-HT1D versus 5-HT1B receptor agonists and, therefore, potential treatments for migraine.
Meng
C Q
CQ
NPS Allelix Corp., Mississauga, Ontario, Canada. cmeng@atherogenics.com
Rakhit
S
S
Lee
D K
DK
Kamboj
R
R
McCallum
K L
KL
Mazzocco
L
L
Dyne
K
K
Slassi
A
A
D003001:Cloning, Molecular; D006801:Humans; D007202:Indicators and Reagents; D008881:Migraine Disorders / Q000188:drug therapy*; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000138:chemical synthesis* / Q000494:pharmacology
C470302:HTR1B protein, human; D007202:Indicators and Reagents; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines