Zaldaride
Title: Zaldaride
CAS Registry Number: 109826-26-8
CAS Name: 1,3-Dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]benzoxazepin-4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-one
Molecular Formula: C26H28N4O2
Molecular Weight: 428.53
Percent Composition: C 72.87%, H 6.59%, N 13.07%, O 7.47%
Literature References: Non-specific ion channel and calmodulin blocker. Prepn: J. W. F. Wasley, J. Norman, EP 233483; eidem, US 4758559 (1987, 1988 both to Ciba-Geigy). Synthesis: S. Boyer et al., J. Heterocycl. Chem. 25, 1003 (1988). Calmodulin inhibition: J. A. Norman et al., Mol. Pharmacol. 31, 535 (1987); and ion channel inhibition: R. Neuhaus, B. F. X. Reber, Eur. J. Pharmacol. 226, 183 (1992). Inhibition of gastric acid secretion: E. W. Black et al., J. Pharmacol. Exp. Ther. 248, 208 (1988); of secretory diarrhea in mice and rats: J. E. Shook et al., ibid. 251, 247 (1989). LC determn in human plasma: D. Chollet, M. Salanon, J. Chromatogr. 593, 73 (1992). Clinical trial in travelers' diarrhea: H. L. DuPont et al., Gastroenterology 104, 709 (1993).
Properties: Crystals, mp 173-175° as hydrate.
Melting point: mp 173-175° as hydrate
 
Derivative Type: Maleate
CAS Registry Number: 109826-27-9
Manufacturers' Codes: CGS-9343B; ZY-17617B
Molecular Formula: C26H28N4O2.C4H4O4
Molecular Weight: 544.60
Percent Composition: C 66.16%, H 5.92%, N 10.29%, O 17.63%
Properties: Crystals, mp 189-190°.
Melting point: mp 189-190°
 
Therap-Cat: Antidiarrheal.
Keywords: Antidiarrheal.

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