Abstract |
Recent studies have demonstrated that selective 5-HT(1F) receptor agonists inhibit neurogenic dural inflammation, a model of migraine headache, indicating that these compounds may be effective therapies for the treatment of migraine pain. This communication describes the synthesis and discovery of a novel compound, N-[3-(2-(dimethylamino)ethyl)-2-methyl-1H-indol-5-yl]-4-fluorobenzamide (4), which possesses high binding affinity and selectivity at the 5-HT(1F) receptor relative to more than 40 other serotonergic and nonserotonergic receptors examined.
|
Authors | Y C Xu, K W Johnson, L A Phebus, M Cohen, D L Nelson, K Schenck, C D Walker, J E Fritz, S W Kaldor, M E LeTourneau, R E Murff, J M Zgombick, D O Calligaro, J E Audia, J M Schaus |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 44
Issue 24
Pg. 4031-4
(Nov 22 2001)
ISSN: 0022-2623 [Print] United States |
PMID | 11708905
(Publication Type: Journal Article)
|
Chemical References |
- Benzamides
- Indoles
- N-(3-(2-dimethylaminoethyl)-2-methyl-1H-indol-5-yl)-4-fluorobenzamide
- Receptors, Neurotransmitter
- Receptors, Serotonin
- Serotonin Receptor Agonists
- serotonin 1F receptor
|
Topics |
- Animals
- Benzamides
(chemical synthesis, chemistry, metabolism, pharmacology)
- Cell Line
- Dura Mater
(drug effects)
- Guinea Pigs
- Humans
- In Vitro Techniques
- Indoles
(chemical synthesis, chemistry, metabolism, pharmacology)
- Inflammation
- Migraine Disorders
(drug therapy)
- Muscle Contraction
(drug effects)
- Muscle, Smooth, Vascular
(drug effects, physiology)
- Rabbits
- Rats
- Receptors, Neurotransmitter
(metabolism)
- Receptors, Serotonin
(drug effects, metabolism)
- Saphenous Vein
(drug effects, physiology)
- Serotonin Receptor Agonists
(chemical synthesis, chemistry, metabolism, pharmacology)
- Structure-Activity Relationship
|