Sumatriptan (GR 43175) interacts selectively with 5-HT1B and 5-HT1D binding sites.
The ability of sumatriptan (GR 43175; 3-[2-dimethylamino]ethyl-N-methyl-1H-indole-5 methane sulphonamide) to interact with 13 neurotransmitter receptor sites was determined using radioligand binding techniques. Sumatriptan displayed the highest affinity for 5-HT1D (Ki = 17 nM) and 5-HT1B (Ki = 27 nM) binding sites and was slightly less potent at 5-HT1A binding sites (Ki = 100 nM). By contrast, sumatriptan was essentially inactive (Ki greater than 10,000 nM) at each of the 10 other binding sites analyzed. These data indicate that sumatriptan interacts selectively with 5-HT1B and 5-HT1D sites and suggest that these interactions may be the basis of its apparent efficacy in the acute treatment of migraine.
Peroutka
S J
SJ
Department of Neurology, Stanford University Medical Center, CA 94305.
McCarthy
B G
BG
D000818:Animals; D002417:Cattle; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D017981:Receptors, Neurotransmitter / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects*; D013449:Sulfonamides / Q000494:pharmacology*; D018170:Sumatriptan; D013552:Swine
D007211:Indoles; D017981:Receptors, Neurotransmitter; D011985:Receptors, Serotonin; D013449:Sulfonamides; D018170:Sumatriptan