Detail of "189188-57-6"

CAS Number:
189188-57-6
Name:
Hydrazinecarboximidamide,2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-
Superlist Name:
Tegaserod maleate
Molecular Structure:
Formula:
C₁₆H₂₃N₅O^.C₄H₄O₄
Molecular Weight:
417.47
Deleted CAS:
173838-31-8
Synonyms:
(2E)-2-[(5-methoxy-1H-indol-3-yl)methylidene]-N-pentylhydrazinecarboximidamide (2Z)-but-2-enedioate (1:1);hydrazinecarboximidamide, 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-, (2E)-, (2Z)-2-butenedioate (1:1);Tegaserod;
Melting Point:
180-183 °C
Boiling Point:
661.4 °C at 760 mmHg
Flash Point:
353.8 °C
Appearance:
white powder

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The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo: The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Beattie, D. T.; Smith, J. A. M.; Marquess, D.; Vickery, R. G.; Armstrong, S. R.; Pulido-Rios, T.; McCullough, J. L.; Sandlund, C.; Richardson, C.; Mai, N.; Humphrey, P. P. A. (Theravance, Inc.There are some reagents with their cas registry numbers 158942-04-2 and 189188-57-6 are used in this study., South San Francisco, CA 94080, USA). British Journal of Pharmacology, 143(5), 549-560 (English) 2004 Nature Publishing Group. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Tegaserod (Zelnorm) is a potent 5-hydroxytryptamine4 (5-HT4) receptor agonist with clin. efficacy in disorders assocd. with reduced gastrointestinal motility and transit. The present study investigated the interaction of tegaserod with 5-HT2 receptors, and compared its potency in this respect to its 5-HT4 receptor agonist activity. Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pKi = 7.5, 8.4 and 7.0, resp.). The 5-HT2B receptor-binding affinity of tegaserod was identical to that at human recombinant 5-HT4(c) receptors (mean pKi = 8.4) in human embryonic kidney-293 (HEK-293) cells stably transfected with the human 5-HT4(c) receptor. Tegaserod (0.1-3 mM) inhibited 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA2 = 8.3), consistent with 5-HT2B receptor antagonist activity. Tegaserod produced, with similar potency, an elevation of adenosine 3',5' cyclic monophosphate in HEK-293 cells stably transfected with the human 5-HT4(c) receptor (mean pEC50 = 8.6), as well as 5-HT4 receptor-mediated relaxation of the rat isolated esophagus (mean pEC50 = 8.2) and contraction of the guinea-pig isolated colon (mean pEC50 = 8.3). Following s.c. administration, tegaserod (0.3 or 1 mg kg-1) inhibited contractions of the stomach fundus in anesthetized rats in response to i.v. dosing of a-Me 5-HT (0.03 mg kg-1) and BW 723C86 (0.3 mg kg-1), selective 5-HT2B receptor agonists. At similar doses, tegaserod (1 and 3 mg kg-1 s.c.) evoked a 5-HT4 receptor-mediated increase in colonic transit in conscious guinea-pigs. The data from this study indicate that tegaserod antagonizes 5-HT2B receptors at concns. similar to those that activate 5-HT4 receptors. It remains to be detd. whether this 5-HT2B receptor antagonist activity of tegaserod contributes to its clin. profile. .

Ion-pair RP-LC of tegaserod maleate and its impurities in pharmaceutical formulations and in dissolution studies: All Rights Reserved. Ion-pair RP-LC of tegaserod maleate and its impurities in pharmaceutical formulations and in dissolution studies. Yang, B.; Gao, M. J.; Duan, G. L. (Department of Pharmaceutical Analysis, School of Pharmacy, Fudan University, Shanghai 200032, Peop. Rep. China). Chromatographia, 63(9-10), 431-436 (English) 2006 Vieweg Verlag/GWV Fachverlage GmbH. CODEN: CHRGB7. ISSN: 0009-5893. DOCUMENT TYPE: Journal CA Section: 64 (Pharmaceutical Analysis) A simple ion-pair reversed-phase high-performance liq. chromatog. (RP-HPLC) method was developed for detn. of tegaserod maleate and related impurities in tablet dosage forms. The mobile phase was (vol.Several substances with their cas registry numbers 189188-57-6 and 10601-19-1 may be metioned in this study./vol.) acetonitrile-25 mmol L-1 sodium dodecyl sulfate, adjusted to pH 2.6 with glacial acetic acid. A C18 column was used as stationary phase and UV detection was at 314 nm. The method was optimized and validated. Response was linearly dependent on concn. between 0.1 and 100 mg mL-1 with a limit of quantification (LOQ) of 0.1 mg mL-1 for tegaserod maleate (S/N = 10). Under optimum conditions, tegaserod maleate was successfully sepd. from related substances, including 5-methoxyindole-3-carboxaldehyde remaining after synthesis and other impurities possibly resulting from oxidization and decompn. The excipients did not interfere with assay of tegaserod maleate in tablet dosage forms. It is suggested that the proposed method can be used for routine quality control and dosage-form assay of tegaserod maleate. .

Detail of "189188-57-6"

Hydrazinecarboximidamide,2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-

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Reference