3544. Eletriptan
Nomenclature
CAS number: 143322-58-1
3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole; 5-[2-(benzenesulfonyl)ethyl]-3-(1-methylpyrrolidin-2(R)-ylmethyl)-1H-indole; UK-116044. C22H26N2O2S; mol wt 382.52.
C 69.08%, H 6.85%, N 7.32%, O 8.37%, S 8.38%.
Description and references
Serotonin 5-HT1B/1D receptor agonist. Prepn: J. E. Macor, M. J. Wythes, WO 9206973; eidem, US 5545644 (1992, 1996 both to Pfizer). Pharmacology: E. Willems et al., Arch. Pharmacol. 358, 212 (1998). Affinity and specificity of receptor binding: C. Napier et al., Eur. J. Pharmacol. 368, 259 (1999). Clinical trial in comparison with sumatriptan, q.v.: P. J. Goadsby et al., Neurology 54, 156 (2000). Review of pharmacokinetics and clinical efficacy: A. Bardsley-Elliot, S. Noble, CNS Drugs 12, 325-333 (1999); of development and clinical experience: G. Sandrini et al., Expert Rev. Neurother. 6, 1413-1421 (2006).
Derivative
Hydrobromide.Nomenclature
CAS number: 177834-92-3
Relpax (Pfizer). C22H26N2O2S.HBr; mol wt 463.43.
C 57.02%, H 5.87%, N 6.04%, O 6.90%, S 6.92%, Br 17.24%.
Properties
White to light pale colored powder. Readily sol in water.Therapeutic Category
Antimigraine.
Keywords
Serotonin Receptor Agonist; Antimigraine