8235. Ritanserin
Nomenclature
CAS number: 87051-43-2
6-[2-[4-[Bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one; R-55667; Tiserton (Janssen). C27H25F2N3OS; mol wt 477.57.
C 67.90%, H 5.28%, F 7.96%, N 8.80%, O 3.35%, S 6.71%.
Description and references
Selective serotonin (5-HT2) receptor antagonist. Prepn: L. E. J. Kennis et al., EP 110435; eidem, US 4533665 (1984, 1985 both to Janssen). Pharmacological profile: F. Awouters et al., Drug Dev. Res. 15, 61 (1988). GC/MS determn in plasma and pharmacokinetics: P. Timmerman et al, Biomed. Environ. Mass Spectrom. 18, 498 (1989). Clinical studies: G. Nappi et al., Headache 30, 439 (1990); G. Bersani et al., Acta Psychiatr. Scand. 83, 244 (1991); J. M. Monti et al., Sleep 16, 647 (1993).
Properties
Crystals from acetonitrile, mp 145.5°. LD50 in male, female mice, rats, dogs (mg/kg): 28.2, 28.2, 20.0, 22.2, 24.1, 33.2 i.v.; 626, 993, 956, 515, ≈1280, 640-1280 orally (Awouters).Derivative
l-Tartrate.Nomenclature
CAS number: 93076-39-2
C27H25F2N3OS.C4H6O6; mol wt 627.66.
C 59.32%, H 4.98%, F 6.05%, N 6.69%, O 17.84%, S 5.11%.
Properties
Solid from 2-propanol, mp 198.7°.Therapeutic Category
Anxiolytic; antidepressant.
Keywords
Antidepressant; Serotonin Receptor Antagonist