Title: Solifenacin
CAS Registry Number: 242478-37-1
CAS Name: (1S)-3,4-Dihydro-1-phenyl-2(1H)-isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester
Additional Names: (1S,3¢R)-3¢quinuclidinyl-1-phenyl-1,2,3,4-tetrahydro-2-isoquinolinecarboxylate
Molecular Formula: C23H26N2O2
Molecular Weight: 362.46
Percent Composition: C 76.21%, H 7.23%, N 7.73%, O 8.83%
Literature References: Muscarinic M3 receptor antagoinst. Prepn: M. Takeuchi et al., WO 9620194; eidem, US 6017927 (1996, 2000 both to Yamanouchi). Receptor binding studies: K. Ikeda et al., Arch. Pharmacol. 366, 97 (2002); selectivity profile: A. Ohtake et al., Eur. J. Pharmacol. 492, 243 (2004). Clinical study in overactive bladder: C. R. Chapple et al., Br. J. Urol. 93, 303 (2004); F. Habb et al., Eur. Urol. 47, 376 (2005). Clinical comparison with tolterodine: C. R. Chapple et al., ibid. 48, 464 (2005). Review of efficacy and tolerability studies: S. Brunton, L. Kuritzky, Curr. Med. Res. Opin. 21, 71-80 (2005); of clinical development: C. K. Payne, Drugs 66, 175-190 (2006).
Properties: Yellow oil.
Derivative Type: Succinate
CAS Registry Number: 242478-38-2
Manufacturers' Codes: YM-905
Trademarks: Vesicare (Yamanouchi)
Molecular Formula: C23H26N2O2.C4H6O4
Molecular Weight: 480.55
Percent Composition: C 67.48%, H 6.71%, N 5.83%, O 19.98%
Properties: White to slightly yellowish crystals, mp ~145°. Freely sol in acetic acid, water, methanol, dimethylsulfoxide.
Melting point: mp ~145°
Therap-Cat: In treatment of urinary incontinence.
Keywords: Antimuscarinic. |