替宁酸
替宁酸结构式
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常用名 | 替宁酸 | 英文名 | Tienilic acid |
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| CAS号 | 40180-04-9 | 分子量 | 331.17 | |
| 密度 | 1.5±0.1 g/cm3 | 沸点 | 534.6±50.0 °C at 760 mmHg | |
| 分子式 | C13H8Cl2O4S | 熔点 | 148-149ºC | |
| MSDS | 中文版 美版 | 闪点 | 277.1±30.1 °C |
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Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.
Expert Opin. Drug Metab. Toxicol. 10(10) , 1313-24, (2014) Drug resistance by Plasmodium falciparum remains a challenge in malaria chemotherapy. This paper will focus on physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid shown to have antimalarial activi... |
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Coupling Laser Diode Thermal Desorption with Acoustic Sample Deposition to Improve Throughput of Mass Spectrometry-Based Screening.
J. Biomol. Screen. 21 , 165-75, (2016) The move toward label-free screening in drug discovery has increased the demand for mass spectrometry (MS)-based analysis. Here we investigated the approach of coupling acoustic sample deposition (ASD) with laser diode thermal desorption (LDTD)-tandem mass sp... |
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Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose.
Chem. Res. Toxicol. 21(9) , 1814-22, (2008) In vitro covalent binding assessments of drugs have been useful in providing retrospective insights into the association between drug metabolism and a resulting toxicological response. On the basis of these studies, it has been advocated that in vitro covalen... |
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Mechanism-based inactivation of cytochrome P450 2C9 by tienilic acid and (+/-)-suprofen: a comparison of kinetics and probe substrate selection.
Drug Metab. Dispos. 37(1) , 59-65, (2009) In vitro experiments were conducted to compare k(inact), K(I) and inactivation efficiency (k(inact)/K(I)) of cytochrome P450 (P450) 2C9 by tienilic acid and (+/-)-suprofen using (S)-flurbiprofen, diclofenac, and (S)-warfarin as reporter substrates. Although t... |
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Kinetics of tienilic acid bioactivation and functional generation of drug-protein adducts in intact rat hepatocytes.
Biochem. Pharmacol. 70(12) , 1870-82, (2005) Drug-induced autoimmune hepatitis is among the most severe hepatic idiosyncratic adverse drug reactions. Considered multifactorial, the disease combines immunological and metabolic aspects, the latter being to date much better known. As for many other model d... |
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Electrospray ionization mass spectrometric analysis of intact cytochrome P450: identification of tienilic acid adducts to P450 2C9.
Biochemistry 38(8) , 2312-9, (1999) A general scheme for the purification of baculovirus-expressed cytochrome P450s (P450s) from the crude insect cell pastes has been designed which renders the P450s suitable for analysis by high-performance liquid chromatography (HPLC) electrospray ionization ... |
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The substrate binding site of human liver cytochrome P450 2C9: an NMR study.
Biochemistry 36(42) , 12672-82, (1997) Purified recombinant human liver cytochrome P450 2C9 was produced, from expression of the corresponding cDNA in yeast, in quantities large enough for UV-visible and 1H NMR experiments. Its interaction with several substrates (tienilic acid and two derivatives... |
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Tienilic acid enhances hyperbilirubinemia in Eisai hyperbilirubinuria rats through hepatic multidrug resistance-associated protein 3 and heme oxygenase-1 induction.
Toxicol. Sci. 91(2) , 651-9, (2006) We demonstrated that tienilic acid, a diuretic drug withdrawn from the market because of hepatic failure, enhanced hyperbilirubinemia in Eisai hyperbilirubinuria rats (EHBR) with a defect of canalicular multidrug resistance-associated protein 2 (Mrp2). In con... |
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Involvement of cytochrome P450-mediated metabolism in tienilic acid hepatotoxicity in rats.
Toxicol. Lett. 183(1-3) , 81-9, (2008) Tienilic acid is reported to be converted into electrophilic metabolites by cytochrome P450 (CYP) in vitro. In vivo, however, the metabolites have not been detected and their effect on liver function is unknown. We previously demonstrated that tienilic acid d... |
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Drug-induced immunotoxicity.
Eur. J. Drug Metab. Pharmacokinet. 23(4) , 443-51, (1998) Immune-related drug responses are one of the most common sources of idiosyncratic toxicity. A number of organs may be the target of such reactions; however, this review concentrates mostly on the liver. Drug-induced hepatitis is generally divided into two cat... |