4900. Iloperidone

Nomenclature

CAS number: 133454-47-4
1-[4-[3-[4-(6-Fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]ethanone; HP-873; ILO-522; Zomaril (Novartis).
C24H27FN2O4; mol wt 426.48.
C 67.59%, H 6.38%, F 4.45%, N 6.57%, O 15.01%.

Description and references

Combined dopamine (D2) and serotonin (5HT2) receptor antagonist. Prepn: J. T. Strupczewski et al., EP 402644; eidem, US 5364866 (1990, 1994 both to Hoechst-Roussel); eidem, J. Med. Chem. 38, 1119 (1995). Pharmacology: M. R. Szewczak et al., J. Pharmacol. Exp. Ther. 274, 1404 (1995). Clinical pharmacokinetics: S. M. Sainati et al., J. Clin. Pharmacol. 35, 713 (1995). HPLC determn in plasma: A. E. Mutlib, J. T. Strupczewski, J. Chromatogr. B 669, 237 (1995). Receptor binding study: S. Kongsamut et al., Eur. J. Pharmacol. 317, 417 (1996). Review of pharmacology and therapeutic potential in schizophrenia: J. M. K. Hesselink, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 2, 71-78 (2000); K. K. Jain, Expert Opin. Invest. Drugs 9, 2935-2943 (2000).

Chemical structure

Properties

Crystals from ethanol, mp 118-120°.

Therapeutic Category

Antipsychotic.

Keywords

Antipsychotic; Benzisoxazoles; Serotonin-Dopamine Antagonist