Ritanserin
Title: Ritanserin
CAS Registry Number: 87051-43-2
CAS Name: 6-[2-[4-[Bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one
Manufacturers' Codes: R-55667
Trademarks: Tiserton (Janssen)
Molecular Formula: C27H25F2N3OS
Molecular Weight: 477.57
Percent Composition: C 67.90%, H 5.28%, F 7.96%, N 8.80%, O 3.35%, S 6.71%
Literature 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).
Melting point: mp 145.5°
Toxicity data: 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 Type: L-Tartrate
CAS Registry Number: 93076-39-2
Molecular Formula: C27H25F2N3OS.C4H6O6
Molecular Weight: 627.66
Percent Composition: 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°.
Melting point: mp 198.7°
 
Therap-Cat: Anxiolytic; antidepressant.
Keywords: Antidepressant; Serotonin Receptor Antagonist.

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