Almotriptan (malate)

Almotriptan is an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (IC50s = 12 and 13 nM, respectively, in a radioligand binding assay). It is selective for human 5-HT1B and 5-HT1D receptors over rat 5-HT1A and human 5-HT2A and 5-HT4 receptors (IC50s = 0.85, 25.1, and 140 µM, respectively). Almotriptan induces contractions in isolated canine saphenous veins (EC50 = 394 nM) but not isolated rabbit renal or mesenteric arteries. It increases carotid vascular resistance in anesthetized cats (ED100 = 11 µg/kg, i.v.) without increasing blood pressure or heart rate. Formulations containing almotriptan have been used in the treatment of migraine headaches.Formal Name: 2-hydroxy-butanedioic acid, compd. with N,N-dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine. CAS Number: 181183-52-8. Synonyms: PNU 180638E. Molecular Formula: C17H25N3O2S . C4H6O5. Formula Weight: 469.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.2 mg/ml, DMSO: 0.1 mg/ml, PBS (pH 7.2): 20 mg/ml. lambdamax: 229 nm. SMILES: CN(C)CCC1=CNC2=CC=C(CS(N3CCCC3)(=O)=O)C=C21.OC(C(O)=O)CC(O)=O. InChi Code: InChI=1S/C17H25N3O2S.C4H6O5/c1-19(2)10-7-15-12-18-17-6-5-14(11-16(15)17)13-23(21,22)20-8-3-4-9-20,5-2(4(8)9)1-3(6)7/h5-6,11-12,18H,3-4,7-10,13H2,1-2H3,2,5H,1H2,(H,6,7)(H,8,9). InChi Key: QHATUKWEVNMHRY-UHFFFAOYSA-N.