Desloratadine - CAS 100643-71-8
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Not Intended for Therapeutic Use. For research use only.
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Histamine Receptor
Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
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SCH-34117, NSC 675447
1.Human UDP-Glucuronosyltransferase (UGT) 2B10: Validation of Cotinine as a Selective Probe Substrate, Inhibition by UGT Enzyme-Selective Inhibitors and Antidepressant and Antipsychotic Drugs, and Structural Determinants of Enzyme Inhibition.
Pattanawongsa A1, Nair PC1, Rowland A1, Miners JO2. Drug Metab Dispos. 2016 Mar;44(3):378-88. doi: 10.1124/dmd.115.068213. Epub 2015 Dec 15.
Although there is evidence for an important role of UGT2B10 in the N-glucuronidation of drugs and other xenobiotics, the inhibitor selectivity of this enzyme is poorly understood. This study sought primarily to characterize the inhibition selectivity of UGT2B10 by UDP-glucuronosyltransferase (UGT) enzyme-selective inhibitors used for reaction phenotyping, and 34 antidepressant and antipsychotic drugs that contain an amine functional group. Initial studies demonstrated that cotinine is a highly selective substrate of human liver microsomal UGT2B10. The kinetics of cotinine N-glucuronidation by recombinant UGT and human liver microsomes (± bovine serum albumin) were consistent with the involvement of a single enzyme. Of the UGT enzyme-selective inhibitors employed for reaction phenotyping, only the UGT2B4/7 inhibitor fluconazole reduced recombinant UGT2B10 activity to an appreciable extent. The majority of antidepressant and antipsychotic drugs screened for effects on UGT2B10 inhibited enzyme activity with IC50 values <100 µM.
2.In Vivo Anti-Inflammatory Effect of H1 Antihistamines in Allergic Rhinitis: A Randomized Clinical Trial.
Bocşan CI1, Bujor AI2, Miron N2, Vesa ŞC1, Deleanu D2, Buzoianu AD2. Balkan Med J. 2015 Oct;32(4):352-8. doi: 10.5152/balkanmedj.2015.15884. Epub 2015 Oct 1.
BACKGROUND: Allergic rhinitis is characterized by a chronic inflammation of nasal mucosa and represents a risk factor for asthma occurrence. H1 antihistamines reduce the symptoms of rhinitis, but some compounds may have anti-inflammatory properties.
3.Detection of metabolic activation leading to drug-induced phospholipidosis in rat hepatocyte spheroids.
Takagi M1, Sanoh S, Santoh M, Ejiri Y, Kotake Y, Ohta S. J Toxicol Sci. 2016;41(1):155-64. doi: 10.2131/jts.41.155.
Drug-induced phospholipidosis (PLD) is one of the adverse reactions to treatment with cationic amphiphilic drugs. Recently, simple and reliable evaluation methods for PLD have been reported. However, the predictive power of these methods for in vivo PLD induction is insufficient in some cases. To accurately predict PLD, we focused on drug metabolism and used three-dimensional cultures of hepatocytes known as spheroids. Here we used the fluorescent phospholipid dye N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)-1,2-dihexadecanoyl-sn-glycero-3-phosphoethanolamine (NBD-PE) to detect PLD induction. After 48 hr exposure to 20 µM amiodarone and amitriptyline, PLD inducers, NBD-PE fluorescence in the spheroids was significantly higher than that in the control. In contrast, 1 mM acetaminophen, as a negative control, did not increase fluorescence. Furthermore, the combination of NBD-PE fluorescence and LysoTracker Red fluorescence and the accumulation of intrinsic phospholipids reflected PLD induction in spheroids.
4.In silico and In vitro evaluation of the anti-inflammatory potential of Centratherum punctatum Cass-A.
Shankaran S K1, Ganai SA1,2, Kp A3, Brindha P3, Mahadevan V1,2. J Biomol Struct Dyn. 2016 Mar 16:1-30. [Epub ahead of print]
Centratherum punctatum Cass, a herb belonging to the family Asteraceae has been traditionally used as a curative against diverse disorders like inflammation, tumour, depression and hypertension. Though the medicinal properties of this plant have been attributed to the presence of flavonoids, glucosides, alkaloids, Vitamin C, etc, the molecular constituents of this plant and of the flavonoids that contribute to its medicinal activity have not been explored yet. This work attempts to evaluate the potential of Centratherum punctatum extract as an anti inflammatory agent. Ethanolic extracts of Centratherum punctatum analysed by High Performance Thin Layer Chromatography (HPTLC) and Liquid Chromatography - Mass Spectrometry (LC-MS/MS) identified the presence of the flavones kaempferol, glycoside Isorhamnetin-3-O-rutinoside and kaempferol-3-glucoside. The plant extract exhibited antioxidant property as confirmed by DPPH assay and IC50 value of 271.
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CAS 100643-71-8 Desloratadine

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