References of 5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrido[4,
3-b]indol-1-one
Title: Alosetron
CAS Registry Number: 122852-42-0
CAS Name: 2,3,4,5-Tetrahydro-5-methyl-2-[(5-methyl-1
H-imidazol-4-yl)methyl]-1
H-pyrido[4,3-
b]indol-1-one
Manufacturers' Codes: GR-68755
Molecular Formula: C17H18N4O
Molecular Weight: 294.35
Percent Composition: C 69.37%, H 6.16%, N 19.03%, O 5.44%
Literature References: Serotonin 5HT3-receptor antagonist. Prepn: I. H. Coates
et al., EP 306323;
eidem, US 5360800 (1989, 1994 both to Glaxo); of isotopically labelled compd: S. R. Prakash
et al., J. Labelled Compd. Radiopharm. 36, 993 (1995). HPLC determn in plasma: T. L. Lloyd
et al., J. Chromatogr. B 678, 261 (1996). Review of clinical pharmacology: M. D. Gunput,
Aliment. Pharmacol. Ther. 13, Suppl. 2, 70-76 (1999); of clinical studies: A. W. Mangel, A. R. Northcutt,
ibid. 77-82. Clinical trial in irritable bowel syndrome: M. Camilleri
et al., Lancet 355, 1035 (2000).
Derivative Type: Hydrochloride
CAS Registry Number: 122852-69-1
Manufacturers' Codes: GR-68755C
Trademarks: Lotronex (GSK)
Molecular Formula: C17H18N4O.HCl
Molecular Weight: 330.81
Percent Composition: C 61.72%, H 5.79%, N 16.94%, O 4.84%, Cl 10.72%
Properties: mp 288-291°.
Melting point: mp 288-291°
Therap-Cat: In treatment of irritable bowel syndrome.
Keywords: Serotonin Receptor Antagonist.