References of 2H-[1,3]Oxazino[3,2-a]indole-10-carboxamide,N-[(1-butyl-4-piperidinyl)methyl]-3,4-dihydro-
Title: Piboserod
CAS Registry Number: 152811-62-6
CAS Name: N-[(1-Butyl-4-piperidinyl)methyl]-3,4-dihydro-2
H-[1,3]oxazino[3,2-
a]indole-10-carboxamide
Manufacturers' Codes: SB-207266
Molecular Formula: C22H31N3O2
Molecular Weight: 369.50
Percent Composition: C 71.51%, H 8.46%, N 11.37%, O 8.66%
Literature References: Selective 5-HT4 receptor antagonist. Prepn: L. M. Gaster, P. A. Wyman,
WO 9318036;
eidem, US 5852014 (1993, 1998 both to SKB).
In vitro and
in vivo studies of bioavailability, pharmacokinetics, and duration: K. A. Wardle
et al., Br. J. Pharmacol. 118, 665 (1996). Effect on gastrointestinal function: G. J. Sanger
et al., Neurogastroenterol. Motil. 10, 271 (1998);
idem et al., Br. J. Pharmacol. 130, 706 (2000). Clinical evaluation in irritable bowel syndrome: L. A. Houghton
et al., Aliment. Pharmacol. Ther. 13, 1437 (1999).
Properties: White solid from ether, mp 110-113°.
Melting point: mp 110-113°
Derivative Type: Hydrochloride
CAS Registry Number: 178273-87-5
Manufacturers' Codes: SB-207266A
Molecular Formula: C22H31N3O2.HCl
Molecular Weight: 405.96
Percent Composition: C 65.09%, H 7.95%, N 10.35%, O 7.88%, Cl 8.73%
Properties: White crystals from ETOH/petrol, mp 254-256° (dec).
Melting point: mp 254-256°
Therap-Cat: Gastroprokinetic
Keywords: Gastroprokinetic; Serotonin Receptor Antagonist.