Title:  Zatebradine 
CAS Registry Number:  85175-67-3 
CAS Name:  3-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one 
Additional Names:  1-(7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-on-3-yl)-3-[N-methyl-N-[2-(3,4-dimethoxyphenyl)ethyl]amino]propane 
Molecular Formula:  C26H36N2O5 
Molecular Weight:  456.57 
Percent Composition:  C 68.40%, H 7.95%, N 6.14%, O 17.52% 
Literature References:  Specific bradycardic agent; sinus node inhibitor.  Prepn:  M. Reiffen et al., EP 65229; eidem, US 4490369 (1982, 1984 both to Thomae); and structure-activity study:  M. Reiffen et al., J. Med. Chem. 33, 1496 (1990).  Pharmacology:  W. Kobinger, C. Lillie, Eur. J. Pharmacol. 104, 9 (1984).  Mechanism of action study:  M. Goethals et al., Circulation 88, 2389 (1993).  Pharmacokinetics:  W. Roth et al., J. Pharm. Sci. 82, 99 (1993).  GC-MS determn in plasma:  J. Schmid et al., J. Chromatogr. 658, 93 (1994). 
  
Derivative Type:  Hydrochloride  
CAS Registry Number:  91940-87-3 
Manufacturers' Codes:  UL-FS-49 
Molecular Formula:  C26H36N2O5.HCl 
Molecular Weight:  493.04 
Percent Composition:  C 63.34%, H 7.56%, N 5.68%, O 16.23%, Cl 7.19% 
Properties:  Two crystalline modifications, mp 188° and mp 168°.  Sol in water. 
Melting point:  mp 188° and mp 168° 
  
Therap-Cat:  Antianginal. 
Keywords:  Antianginal; Bradycardic Agent.   |