Title: Sarizotan
CAS Registry Number: 351862-32-3
CAS Name: N-[[(2R)-3,4-Dihydro-2H-1-benzopyran-2-yl]methyl]-5-(4-fluorophenyl)-3-pyridinemethanamine
Additional Names: (R)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chromane; (R)-(-)-1-N-[5-(4-fluorophenyl)-3-pyridylmethyl]-N-2-chromanylmethylamine
Manufacturers' Codes: EMD-77697
Molecular Formula: C22H21FN2O
Molecular Weight: 348.41
Percent Composition: C 75.84%, H 6.08%, F 5.45%, N 8.04%, O 4.59%
Literature References: Dual serotonin 5-HT1A receptor agonist and dopamine D2 receptor antagonist. Prepn: H. Böttcher et al., EP 707007; eidem, US 5767132 (1996, 1998 both to Merck Patent GmbH). PET receptor binding study: E. A. Rabiner et al., J. Psychopharmacol. 16, 195 (2002). Neurochemical profile: G. D. Bartoszyk et al., J. Neural Transm. 111, 113 (2004). Clinical evaluation in dyskinesia in Parkinson's disease: C. W. Olanow et al., Clin. Neuropharmacol. 27, 58 (2004); W. Bara-Jimenez et al., Mov. Disord. 20, 932 (2005).
Derivative Type: Dihydrochloride
CAS Registry Number: 177976-12-4
Manufacturers' Codes: EMD-128130
Molecular Formula: C22H21FN2O.2HCl
Molecular Weight: 421.34
Percent Composition: C 62.71%, H 5.50%, F 4.51%, N 6.65%, O 3.80%, Cl 16.83%
Properties: mp 234-235°. [a]20 -65° (c = 1 in methanol).
Melting point: mp 234-235°
Optical Rotation: [a]20 -65° (c = 1 in methanol)
Therap-Cat: Antidyskinetic.
Keywords: Antidyskinetic; Serotonin Receptor Agonist; Dopamine Receptor Antagonist. |