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Sumatriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 9.3 and 7.3 nM, respectively). It also binds to the 5-HT1F receptor (IC50 = 17.8 nM). It induces vasoconstriction in isolated human middle meningeal arteries (EC50 = 89.9 nM), an effect that can be reduced by the 5-HT1B/1D receptor antagonists GR125,743 and GR127,935. Sumatriptan reduces acute, but not chronic, mechanical hyperalgesia in a mouse model of pain induced by nitroglycerin, which is a known migraine trigger in humans. Formulations containing sumatriptan have been used in the treatment of migraine headache.Formal Name: butanedioic acid, compd. with 3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamide. CAS Number: 103628-48-4. Synonyms: GR 43175C. Molecular Formula: C14H21N3O2S . C4H6O4. Formula Weight: 413.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 230, 285 nm. SMILES: CN(C)CCC1=CNC2=CC=C(CS(NC)(=O)=O)C=C21.O=C(CCC(O)=O)O. InChi Code: InChI=1S/C14H21N3O2S.C4H6O4/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3,5-3(6)1-2-4(7)8/h4-5,8-9,15-16H,6-7,10H2,1-3H3,1-2H2,(H,5,6)(H,7,8). InChi Key: PORMUFZNYQJOEI-UHFFFAOYSA-N.
Keywords:
GR 43175C, 3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulfonamide-butanedioic acid
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