4536. Granisetron

Nomenclature

CAS number: 109889-09-0
1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide.
C18H24N4O; mol wt 312.41.
C 69.20%, H 7.74%, N 17.93%, O 5.12%.

Description and references

Specific serotonin (5HT3) receptor antagonist. Prepn: F. D. King, EP 200444; idem, US 4886808 (1986, 1989 both to Beecham). 5HT3 receptor binding study: G. J. Kilpatrick et al., Nature 330, 746 (1987). Series of articles on pharmacology and clinical trials to prevent chemotherapy-induced emesis: Semin. Oncol. 22, Suppl. 10, 1-30 (1995).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 107007-99-8
BRL-43694A; Kytril (SKB).
C18H24N4O.HCl; mol wt 348.87.
C 61.97%, H 7.22%, N 16.06%, O 4.59%, Cl 10.16%.

Properties

White to off-white solid, mp 290-292°. Readily sol in water at 20°.

Therapeutic Category

Antiemetic.

Keywords

Antiemetic; Serotonin Receptor Antagonist