308. Alosetron

Nomenclature

CAS number: 122852-42-0
2,3,4,5-Tetrahydro-5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-1H-pyrido[4,3-b]indol-1-one; GR-68755.
C17H18N4O; mol wt 294.35.
C 69.37%, H 6.16%, N 19.03%, O 5.44%.

Description and 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).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 122852-69-1
GR-68755C; Lotronex (GSK).
C17H18N4O.HCl; mol wt 330.81.
C 61.72%, H 5.79%, N 16.94%, O 4.84%, Cl 10.72%.

Properties

mp 288-291°.

Therapeutic Category

In treatment of irritable bowel syndrome.

Keywords

Serotonin Receptor Antagonist