Zuclopenthixol-Z-Clopenthixol-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZuclopenthixolCat. No.: HY-A0163CAS No.: 53772-83-1Synonyms: (Z)-Clopenthixol分式: CHClNOS分量: 400.96作靶點(diǎn): Dopamine Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mont

2、h溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 150 mg/mL (374.10 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.4940 mL 12.4701 mL 24.9401 mL5 mM 0.4988 mL 2.4940 mL 4.9880 mL10 mM 0.2494 mL 1.2470 mL 2.4940 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Zuc

3、lopenthixol種噻噸衍物，它是多巴胺D1/D2受體 (dopamine D1/D2 receptor) 的拮抗劑。IC50 & Target D1/D2 receptor 1.體內(nèi)研究After acute treatment, Zuclopenthixol (0.2 and 0.4 mg/kg)-treated animals exhibit ethopharmacological1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEprofiles characterized by a decrease in offensive beha

4、viors without impairment of motor activity (0.2 mg/kg).In contrast, the antiaggressive action of the highest dose used (0.4 mg/kg) is accompanied by a markedincrease of immobility. After subchronic treatment, no tolerance to Zuclopenthixol antiaggressive or motoractivity is observed 1.Administration

5、 of Zuclopenthixol (0.7 and 1.4 mg/kg) significantly elevate MDA level compared to respectivecontrols. Nevertheless, there is no difference between the two dose levels with respect to their effect on ratbrain MDA level. Post hoc pairwise comparisons between the means of groups (n=12) receiving diffe

6、rentdose levels of Zuclopenthixol reveal that administration of 1.4 mg/kg of Zuclopenthixol significantly reducesGSH level compared to both vehicle-treated and Zuclopenthixol (0.7 mg/kg)-treated animals (P 2.PROTOCOLAnimal Mice 1Administration Zuclopenthixol (0.025-0.4 mg/kg) is administered acutely

7、 or subchronically for 10 days, on agonistic behaviorelicited by isolation in male mice. Individually housed mice are exposed to anosmic standard opponents 30min after the drug administration, and encounters are videotaped and evaluated using an ethologically basedanalysis 1.Rats 2Male albino rats o

8、f Wistar strain weighing 200-250 g are used. They are kept in a temperature of 23-25Cwith alternating 12-hour light and dark cycles and allowed free access to food and water. Animals are dividedinto six groups (n=6). Two groups receive two dose levels of Zuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 mi

9、nand SCO (1.4 mg/kg i.p.) 30 min before decapitation. A third group of rats is injected with saline, with thesame content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the test solution, 60 min and then SCO (1.4mg/kg i.p.) 30 min before decapitation. The forth and fifth groups of rats receive

10、 two dose levels ofZuclopenthixol (0.7 and 1.4 mg/kg i.p.) 60 min and saline 30 min before decapitation. A control group of sixanimals is given saline, with the same content of ethanol (20% v/v) and vegetable oil (2.8% v/v) in the testsolution, 60 min and then saline 30 min before decapitation and i

11、s run concurrently with drug-treated groups2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Manzaneque JM, et al. An ethopharmacological assessment of the effects of zuclopenthixol on agonistic interactions in male mice.Methods Find Exp Clin Pharmacol. 1999 Jan-Feb;21(1):11-5.2. Khalifa AE, et al. Pro-oxidant activity of zuclopenthixol in vivo: differential effect of the drug on brain oxidative status of scopolamine-treated rats. Hum Exp Toxicol. 2004 Aug;23(9):439-45.McePdfHeightCaution: Prod