4207. Fluspirilene

Nomenclature

CAS number: 1841-19-6
8-[4,4-Bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one; R-6128; Imap (McNeil); Redeptin (SK & F).
C29H31F2N3O; mol wt 475.57.
C 73.24%, H 6.57%, F 7.99%, N 8.84%, O 3.36%.

Description and references

Prepn: BE 633914; P. A. J. Janssen, US 3238216 (1963, 1966 both to Janssen). HPLC determn: A. H. Hikal, H. I. Al-Shoura, J. Liq. Chromatogr. 5, 2205 (1982). Metabolism in rat: J. P. P. Heykants, Life Sci. 8, Part I, 1029 (1969). Pharmacology: P. A. J. Janssen et al., Arzneim.-Forsch. 20, 1689 (1970). Calcium channel blocking activity: R. J. Gould et al., Proc. Natl. Acad. Sci. USA 80, 5122 (1983); J. P. Galizzi et al., ibid. 83, 7513 (1986). Clinical trials in schizophrenia: H. Immich et al., Arzneim.-Forsch. 20, 1699 (1970); G. Chouinard et al., J. Clin. Psychopharmacol. 6, 21 (1986).

Chemical structure

Properties

White to yellowish amorphous or crystalline solid, mp 187.5-190°. Soly in water: 0.015-0.020 mg/ml. LD50 i.m. in rats: 146 ±14 mg/kg (Janssen).

Therapeutic Category

Antipsychotic.

Keywords

Antipsychotic