Title: Tegaserod
CAS Registry Number: 145158-71-0
CAS Name: 2-[(5-Methoxy-1
H-indol-3-yl)methylene]-
N-pentylhydrazinecarboximidamide
Molecular Formula: C16H23N5O
Molecular Weight: 301.39
Percent Composition: C 63.76%, H 7.69%, N 23.24%, O 5.31%
Literature References: Selective serotonin 5HT4-receptor partial agonist. Prepn: R. K. A. Giger, H. Mattes,
EP 505322;
eidem, US 5510353 (1992, 1996 both to Sandoz); K.-H. Buchheit
et al., J. Med. Chem. 38, 2331 (1995). Clinical pharmacology: S. Appel
et al., Clin. Pharmacol. Ther. 62, 546 (1997); and pharmacokinetics:
idem et al., J. Clin. Pharmacol. 37, 229 (1997). Clinical trial in irritable bowel syndrome: S. A. Müller-Lissner
et al., Aliment. Pharmacol. Ther. 15, 1655 (2001); in female patients: J. Novick
et al., ibid. 16, 1877 (2002). Review of clinical efficacy: B. W. Jones
et al., J. Clin. Pharm. Ther. 27, 343-352 (2002); of mechanism of action, efficacy and safety: M. Corsetti, J. Tack,
Expert Opin. Pharmacother. 3, 1211-1218 (2002).
Properties: mp 155°.
Melting point: mp 155°
Derivative Type: Maleate
CAS Registry Number: 189188-57-6
Manufacturers' Codes: SDZ-HTF-919
Trademarks: Zelmac (Novartis); Zelnorm (Novartis)
Molecular Formula: C16H23N5O.C4H4O4
Molecular Weight: 417.46
Percent Composition: C 57.54%, H 6.52%, N 16.78%, O 19.16%
Therap-Cat: Gastroprokinetic; in treatment of irritable bowel syndrome.
Keywords: Gastroprokinetic; Serotonin Receptor Agonist.