Ketanserin-tartrate-R41468-tartrate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKetanserin tartrateCat. No.: HY-10562ACAS No.: 83846-83-7Synonyms: R41468 tartrate分式: CHFNO分量: 545.51作靶点: 5-HT Receptor; Potassium Channel; Autophagy作通路: GPCR/G Protein; Neuronal Signaling; MembraneTransporter/Ion Channel; Autop

2、hagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 150 mg/mL (274.97 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.58 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂

3、师www.MedChemESolubility: 2.5 mg/mL (4.58 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.58 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ketanserin tartrate种选择性的 5-HT receptor 拮抗剂。Ketanserin tartrate 也抑制 hERG 电流 (IhERG)，IC50 为 0.11 M，这种作具有浓度依赖性。IC50 & Target IC50: 0.11 M

4、(hERG current) 1IC50: 15223 M (5-HT receptor) 2体外研究 Ketanserin at 0.3 M inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) ofhERG channels with a 5-min exposure 1. The synergistic effect observed for AA with 5-HT is, also, blockedby the 5-HT receptor blockers cypr

5、oheptadine (IC50=22.07 M), Ketanserin (IC50=15223 M). Ketanserin(50-350 M) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value ofCyproheptadine is 227 M and Ketanserin is 15223 M 2. Ketanserin inhibits platelet aggregation with anIC50 of 240 (169-339) nM 3.体内研究

6、 Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels innumerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus,dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrainperiaq

7、ueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in variousbrain regions 4.PROTOCOLCell Assay 1 The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbeccos modifiedEagles medium (DMEM) supplemented with 10% foetal bovine serum, 400

8、 g/mL G418. The HEK 293 cellline stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained inDMEM containing 10% foetal bovine serum and 100 g/mL hygromycin. Cells used for electrophysiology areseeded on a glass coverslip. The mutant hERG channels are constructed, a

9、nd are transiently expressed inHEK 293 cells using 10 L of Lipofectamine 2000 with 4 g of hERG mutant cDNA in pCDNA3 vector 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rat 4Administration 4 A total of 155 specific-pathogen-free 2-month-old

10、male Sprague-Dawley rats, weighing 180-220 g, are used.The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group(DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2Areceptor agonist (DOI) PS group (DOI-PS gr

11、oup, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group(Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group);and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are2/3 Master of Small Molecules 您边的抑制剂师www

12、.MedChemEfurther divided into six subgroups (n=5 each) according to the time between the stress and analysis;immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normalfeed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is in

13、jected intraperitoneallyat 5 mg/kg at 1 hour before each stress exposure.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Tang Q, et al. The 5-HT2 antagonist Ketanserin is an open channel blocker of human cardiac ether-go-go-related gene (hE

14、RG)potassium channels. Br J Pharmacol. 2008 Oct;155(3):365-73.2. Khan N, et al. Investigation of cyclooxygenase and signaling pathways involved in human platelet aggregation mediated by synergisticinteraction of various agonists. Drug Des Devel Ther. 2015 Jul 6;9:3497-506.3. Kekewska A, et al. Antis

15、erotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells. J Pharmacol ExpTher. 2012 Feb;340(2):369-76.4. Jiang DG, et al. Serotonin regulates brain-derived neurotrophic factor expression in select brain regions during acute psychologicalstress. Neural Regen Res.