1319. Blonanserin

Nomenclature

CAS number: 132810-10-7
2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine; AD-5423; Lonasen (Dainippon).
C23H30FN3; mol wt 367.50.
C 75.17%, H 8.23%, F 5.17%, N 11.43%.

Description and references

Dopamine D2 and serotonin 5-HT2 receptor antagonist. Prepn: K. Hino et al., EP 385237; eidem, US 5021421 (1990, 1991 both to Dainippon). HPLC determn in plasma: M. Matsuda et al., J. Pharm. Biomed. Anal. 15, 1449 (1997). X-ray crystal structure: K. Suzuki et al., Anal. Sci. 18, 1289 (2002). In vitro receptor binding study and in vivo pharmacology in animals: M. Oka et al., J. Pharmacol. Exp. Ther. 264, 158 (1993). Evaluation in mouse models of schizophrenia: T. Nagai et al., NeuroReport 14, 269 (2003). Review of development and clinical experience: C. E. Heading, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 2, 79-84 (2002).

Chemical structure

Properties

Crystals from acetonitrile, mp 123-124°.

Therapeutic Category

Antipsychotic.

Keywords

Antipsychotic; Serotonin-Dopamine Antagonist