Title: Riluzole
CAS Registry Number: 1744-22-5
CAS Name: 6-(Trifluoromethoxy)-2-benzothiazolamine
Synonyms: 2-amino-6-(trifluoromethoxy)benzothiazole
Manufacturers' Codes: PK-26124; RP-54274
Trademarks: Rilutek (Aventis)
Molecular Formula: C8H5F3N2OS
Molecular Weight: 234.20
Percent Composition: C 41.03%, H 2.15%, F 24.34%, N 11.96%, O 6.83%, S 13.69%
Literature References: Modulates glutamatergic transmission. Prepn: L. M. Yagupol'skii, L. Z. Gandel'sman,
Zh. Obshch. Khim. 33, 2301 (1963),
C.A. 60, 692a (1964). Prepd but not claimed: J. Mizoule,
EP 50551;
idem, US 4370338 (1982, 1983 both to Pharmindustrie). Pharmacology: J. Mizoule
et al., Neuropharmacology 24, 767 (1985); F. Wahl
et al., Eur. J. Pharmacol. 230, 209 (1993). Mechanism of action studies: M.-W. Debono
et al., ibid. 235, 283; D. Martin
et al., ibid. 250, 473. Use in treatment of motor nerve diseases: E. Louvel,
EP 558861 (1993 to Rh?ne-Poulenc Rorer). Clinical study in amyotrophic lateral sclerosis: G. Bensimon
et al., N. Engl. J. Med. 330, 585 (1994). Review: J. Wokke,
Lancet 348, 795-799 (1996).
Properties: Crystals from ethanol/water (1:1), mp 119°. LD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule).
Melting point: mp 119°
Toxicity data: LD50 in mice (mg/kg): 46 i.p.; 67 orally (Mizoule)
Therap-Cat: Neuroprotective.
Keywords: Neuroprotective.