Title: Zotepine
CAS Registry Number: 26615-21-4
CAS Name: 2-[(8-Chlorodibenzo[b,f]thiepin-10-yl)oxy]-N,N-dimethylethanamine
Additional Names: 2-chloro-11-(2-dimethylaminoethoxy)dibenzo[b,f]thiepine
Trademarks: Lodopin (Fujisawa); Nipolept (Aventis); Setous (Shionogi); Zoleptil (Abbott)
Molecular Formula: C18H18ClNOS
Molecular Weight: 331.86
Percent Composition: C 65.15%, H 5.47%, Cl 10.68%, N 4.22%, O 4.82%, S 9.66%
Literature References: Combined dopamine (D2) and serotonin (5-HT2) receptor antagonist. Prepn: S. Umio et al., DE 1907670; eidem, US 3704245 (1969, 1972 both to Fujisawa); I. Ueda et al., Chem. Pharm. Bull. 26, 3058 (1978). Pharmacology: S. Uchida et al., Arzneim.-Forsch. 29, 1588 (1979). Pharmacokinetics and metabolism: K. Noda et al., ibid. 1595. Toxicology: K. Fukuhara et al., ibid. 1600. Effects on serotonin receptors: A. Czyrak et al., Pharmacopsychiatry 26, 53 (1993). GC-MS determn in plasma: O. Tanaka et al., Ther. Drug Monit. 18, 294 (1996). Clinical trials in schizophrenia: C. Barnas et al., Int. Clin. Psychopharmacol. 7, 23 (1992); A. Meyer-Lindenberg et al., Pharmacopsychiatry 30, 35 (1997).
Properties: Crystals from cyclohexane, mp 90-91°. uv max (95% ethanol): 266 nm. LD50 in male mice, rats (mg/kg): 108, 458 orally; 43.3, 39.7 i.v.; 40.0, 97.0 i.p.; 84.9, 2080 s.c. (Fukuhara).
Melting point: mp 90-91°
Absorption maximum: uv max (95% ethanol): 266 nm
Toxicity data: LD50 in male mice, rats (mg/kg): 108, 458 orally; 43.3, 39.7 i.v.; 40.0, 97.0 i.p.; 84.9, 2080 s.c. (Fukuhara)
Therap-Cat: Antipsychotic.
Keywords: Antipsychotic; Other Tricyclics; Serotonin-Dopamine Antagonist. |