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.
MeSH terms
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Animals
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Benzamides / chemical synthesis*
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Benzamides / chemistry
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Benzamides / metabolism
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Benzamides / pharmacology
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Cell Line
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Dura Mater / drug effects
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Guinea Pigs
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Humans
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In Vitro Techniques
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / metabolism
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Indoles / pharmacology
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Inflammation
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Migraine Disorders / drug therapy*
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Muscle Contraction / drug effects
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Muscle, Smooth, Vascular / drug effects
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Muscle, Smooth, Vascular / physiology
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Rabbits
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Rats
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Receptor, Serotonin, 5-HT1F
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Receptors, Neurotransmitter / metabolism
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Receptors, Serotonin / drug effects*
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Receptors, Serotonin / metabolism
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Saphenous Vein / drug effects
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Saphenous Vein / physiology
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Serotonin Receptor Agonists / chemical synthesis*
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Serotonin Receptor Agonists / chemistry
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Serotonin Receptor Agonists / metabolism
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Serotonin Receptor Agonists / pharmacology
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Structure-Activity Relationship
Substances
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Benzamides
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Indoles
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N-(3-(2-dimethylaminoethyl)-2-methyl-1H-indol-5-yl)-4-fluorobenzamide
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Receptors, Neurotransmitter
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Receptors, Serotonin
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Serotonin Receptor Agonists