Tegaserod maleate5-HT4 partial agonist CAS# 189188-57-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 189188-57-6 | SDF | Download SDF |
| PubChem ID | 135413539 | Appearance | Powder |
| Formula | C20H27N5O5 | M.Wt | 417.46 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 35 mg/mL (83.84 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | (Z)-but-2-enedioic acid;1-[(E)-(5-methoxy-1H-indol-3-yl)methylideneamino]-2-pentylguanidine | ||
| SMILES | CCCCCN=C(N)NN=CC1=CNC2=C1C=C(C=C2)OC.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | CPDDZSSEAVLMRY-FEQFWAPWSA-N | ||
| Standard InChI | InChI=1S/C16H23N5O.C4H4O4/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15;5-3(6)1-2-4(7)8/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21);1-2H,(H,5,6)(H,7,8)/b20-11+;2-1- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Partial agonist of 5-HT4 (Ki = 12 nM). |
Tegaserod maleate Dilution Calculator
Tegaserod maleate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3954 mL | 11.9772 mL | 23.9544 mL | 47.9088 mL | 59.886 mL |
| 5 mM | 0.4791 mL | 2.3954 mL | 4.7909 mL | 9.5818 mL | 11.9772 mL |
| 10 mM | 0.2395 mL | 1.1977 mL | 2.3954 mL | 4.7909 mL | 5.9886 mL |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4791 mL | 0.9582 mL | 1.1977 mL |
| 100 mM | 0.024 mL | 0.1198 mL | 0.2395 mL | 0.4791 mL | 0.5989 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Estimation of tegaserod maleate by differential pulse polarography.[Pubmed:20177456]
Indian J Pharm Sci. 2009 Jan;71(1):50-2.
A highly sensitive differential pulse polarographic method has been developed for the estimation of Tegaserod maleate after treating it with hydrogen peroxide solution. The oxidation of Tegaserod maleate is a reversible process as the oxidized product could be reduced at hanging mercury drop electrode in a quantitative manner using differential pulse polarography mode. The limit of quantification was 0.1ng/ml. The voltametric peak was obtained at -1.05 volts in presence of 0.1M potassium chloride as supporting electrolyte. The technique could be used successfully to analyze Tegaserod maleate in its tablet formulation.
Tegaserod maleate in the treatment of irritable bowel syndrome: a clinical review.[Pubmed:12946544]
Clin Ther. 2003 Jul;25(7):1952-74.
BACKGROUND: Approved in July 2002, Tegaserod maleate is a partial 5-hydroxytryptamine 4-receptor agonist used to improve symptoms of constipation-predominant irritable bowel syndrome (IBS). The physiologic actions of tegaserod relate to its ability to stimulate gastric and intestinal motility. OBJECTIVE: This article reviews available data on the pharmacokinetic and pharmacodynamic properties and clinical efficacy of tegaserod. METHODS: Searches of MEDLINE and PubMed from 1966 to the present were conducted using the search terms tegaserod, Tegaserod maleate, irritable bowel syndrome, and Rome criteria. Abstracts presented at national meetings between 1997 and 2002 were reviewed and included if perceived to be reliable and relevant. RESULTS: In clinical trials, tegaserod was associated with significantly better scores on the subject's global assessment of relief compared with placebo (P < 0.05). The absolute efficacy of tegaserod compared with placebo varied between trials and averaged 10% to 12%. Tegaserod had a good safety profile; diarrhea was the only adverse effect that occurred more often in tegaserod recipients than in placebo recipients. No electrocardiographic changes were observed at therapeutic concentrations of tegaserod. Long-term (1-year) treatment with tegaserod appeared to be well tolerated. The recommended dosage for patients aged >18 years with constipation-predominant IBS is 6 mg PO BID before meals for 4 to 6 weeks, with an additional 4 to 6 weeks of treatment if initial therapy is partially effective. CONCLUSIONS: The addition of tegaserod to the arsenal of moderately effective medication currently used in the treatment of IBS may be helpful in patients with constipation-predominant IBS. Continuous postmarketing surveillance and reporting of adverse reactions are essential to further characterize the safety profile of this new agent.
In vitro and in vivo evaluation of tegaserod maleate pH-dependent tablets.[Pubmed:18037278]
Eur J Pharm Biopharm. 2008 May;69(1):247-54.
The purpose of this study was to prepare Tegaserod maleate (TM) pH-dependent tablets and evaluate their advantages as a sustained release delivery system. TM, insoluble in water and unstable in gastric milieu, was formulated into pH-dependent tablets coated with combinations of two methacrylic acid copolymers - Eudragit L100 and Eudragit S100. The influence of core tablet compositions, polymer combination ratios and coating levels on the in vitro release rate of TM from coated tablets was investigated. The optimum formulation was evaluated for in vitro release rate and in vivo bioavailability study on beagle dogs. In addition, physico-chemical properties of the drug, including solubility at different pH and temperatures, and dissociation constant were determined. The results showed that no drug was released in 0.1 mol/L hydrochloric acid within 2h, and about 90% of the drug was released in the pH 6.8 phosphate buffer within 12h in a sustained manner. The pharmacokinetic investigation showed that TM pH-dependent tablets exhibited a sustained plasma concentration, a lag time of approximately 2.3h and a relative bioavailability of 159% compared to plain tablets. A close correlation existed between the in vitro release rate of the pH-dependent system and its in vivo absorption percentage. The results of the present study have demonstrated that the pH-dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric milieu and improving oral bioavailability of TM for the treatment of irritable bowel syndrome.
The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.[Pubmed:7608899]
J Med Chem. 1995 Jun 23;38(13):2331-8.
A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonist described so far (EC50 = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, Ki = 12 nM) to and 300-fold higher (1h, Ki = 0.04 nM) than serotonin.
