Title: Olopatadine
CAS Registry Number: 113806-05-6
CAS Name: (11
Z)-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.
