304. Almotriptan

Nomenclature

CAS number: 154323-57-6
N,N-Dimethyl-5-[(1-pyrrolidinylsulfonyl)methyl]-1H-indole-3-ethanamine; 1-[[[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine; 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulfonyl]pyrrolidine; LAS-31416.
C17H25N3O2S; mol wt 335.46.
C 60.87%, H 7.51%, N 12.53%, O 9.54%, S 9.56%.

Description and references

Serotonin 5HT1B/1D-receptor agonist. Prepn: D. F. Forner et al., WO 9402460; eidem, US 5565447 (1994, 1996 both to Almirall). Clinical pharmacokinetics: J. C. Fleishaker et al., Clin. Pharmacol. Ther. 67, 498 (2000). Review of pharmacology: F. Kamali, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 2, 197-202 (2000); of clinical studies: D. W. Dodick, Expert Opin. Pharmacother. 4, 1157-1163 (2003).

Chemical structure

Derivative

Maleate.

Nomenclature

CAS number: 181183-52-8
PNU-180638E; Almogran (Almirall); Axert (Pharmacia & Upjohn).
C17H25N3O2S.C4H6O5; mol wt 469.55.
C 53.72%, H 6.65%, N 8.95%, O 23.85%, S 6.83%.

Properties

White to slightly yellow crystalline powder; sol in water.

Therapeutic Category

Antimigraine.

Keywords

Antimigraine; Serotonin Receptor Agonist