Title:  Olopatadine 
CAS Registry Number:  113806-05-6 
CAS Name:  (11Z)-11-[3-(Dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid 
Molecular Formula:  C21H23NO3 
Molecular Weight:  337.41 
Percent Composition:  C 74.75%, H 6.87%, N 4.15%, O 14.23% 
Literature References:  Dual acting histamine H1-receptor antagonist and mast cell stabilizer.  Prepn:  E. Oshima et al., EP 235796; eidem, US 5116863 (1987, 1992 both to Kyowa); eidem, J. Med. Chem. 35, 2074 (1992).  Pharmacology:  C. Kamei et al., Arzneim.-Forsch. 45, 1005 (1995); J. M. Yanni et al., J. Ocul. Pharmacol. Ther. 12, 389 (1996).  Receptor binding profile:  N. A. Sharif et al., J. Pharmacol. Exp. Ther. 278, 1252 (1996).  Clinical trial in allergic conjunctivitis:  M. B. Abelson, L. Spitalny, Am. J. Ophthalmol. 125, 797 (1998). 
Properties:  Crystallized as the hemihydrate from 2-propanol + water, mp 188-189.5°. 
Melting point:  mp 188-189.5° 
  
Derivative Type:  Hydrochloride  
CAS Registry Number:  140462-76-6 
Manufacturers' Codes:  AL-4943A;  KW-4679 
Trademarks:  Opatanol (Alcon);  Patanol (Alcon) 
Molecular Formula:  C21H23NO3.HCl 
Molecular Weight:  373.87 
Percent Composition:  C 67.46%, H 6.47%, N 3.75%, O 12.84%, Cl 9.48% 
Properties:  Crystals from acetone-water, mp 248° (dec).  Sol in water. 
Melting point:  mp 248° (dec) 
  
Therap-Cat:  Antiallergic; antihistaminic. 
Keywords:  Antihistaminic; Tricyclics; Other Tricyclics.   |