Itasetron
Title: Itasetron
CAS Registry Number: 123258-84-4
CAS Name: 2,3-Dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-2-oxo-1H-benzimidazole-1-carboxamide
Additional Names: 2-oxo-N-1aH,5aH-tropan-3a-yl-1-benzimidazoline-1-carboxamide
Molecular Formula: C16H20N4O2
Molecular Weight: 300.36
Percent Composition: C 63.98%, H 6.71%, N 18.65%, O 10.65%
Literature References: Serotonin (5-HT3) receptor antagonist. Prepn: M. Turconi et al., EP 309423 (1989 to Istituto De Angeli); eidem, US 5223511 (1993 to Boehringer, Ing.); M. Turconi et al., J. Med. Chem. 33, 2101 (1990). Pharmacology: idem et al., Eur. J. Pharmacol. 203, 203 (1991). Mode of action: M. B. Passani et al., Br. J. Pharmacol. 112, 695 (1994). Clinical efficacy and tolerability: H. Goldschmidt et al., Anti-Cancer Drugs 8, 436 (1997). Review of therapeutic potential: M. B. Passani, R. Corradetti, CNS Drug Reviews 2, 195-213 (1996).
Properties: Crystals from acetonitrile, mp 205-207°. LD50 in mice, rats (mg/kg): 56, 62 i.v. (Passani).
Melting point: mp 205-207°
Toxicity data: LD50 in mice, rats (mg/kg): 56, 62 i.v. (Passani)
 
Derivative Type: Hydrochloride
CAS Registry Number: 127618-28-4
Manufacturers' Codes: DAU 6215
Molecular Formula: C16H20N4O2.HCl
Molecular Weight: 336.82
Percent Composition: C 57.05%, H 6.28%, N 16.63%, O 9.50%, Cl 10.53%
Properties: Colorless crystals, mp 270°.
Melting point: mp 270°
 
Therap-Cat: Antiemetic.
Keywords: Antiemetic; Serotonin Receptor Antagonist.

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