6822. Olanzapine

Nomenclature

CAS number: 132539-06-1
2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine; LY-170053; Zyprexa (Lilly).
C17H20N4S; mol wt 312.43.
C 65.35%, H 6.45%, N 17.93%, S 10.26%.

Description and references

Serotonin (5-HT2) and dopamine (D1/D2) receptor antagonist with anticholinergic activity. Prepn: J. K. Chakrabarti et al., EP 454436; eidem, US 5229382 (1991, 1993 both to Lilly). Comparative pharmacology: N. A. Moore et al., Curr. Opin. Investig. Drugs 2, 281 (1993). HPLC determn in human plasma: J. T. Catlow et al., J. Chromatogr. B 668, 85 (1995). Clinical evaluation in schizophrenia: D. S. Baldwin, S. A. Montgomery, Int. Clin. Psychopharmacol. 10, 239 (1995); in mania of bipolar disorder: M. Tohen et al., Am. J. Psychiatry 156, 702 (1999). Review of pharmacology and clinical experience: B. C. Lund, P. J. Perry, Expert Opin. Pharmacother. 1, 305-323 (2000).

Chemical structure

Properties

Crystals from acetonitrile, mp 195°. Practically insol in water.

Therapeutic Category

Antipsychotic.

Keywords

Antipsychotic; Other Tricyclics; Serotonin-Dopamine Antagonist