1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEScopolamine hydrobromideCat. No.: HY-N0296ACAS No.: 114-49-8Synonyms: (-)-Scopolamine hydrobromide; Hyoscine hydrobromide;Scopine hydrobromide分式: CHBrNO分量: 384.26作靶點: mAChR; 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存

2、式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 H2O : 100 mg/mL (260.24 mM)DMSO : 32 mg/mL (83.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6024 mL 13.0120 mL 26.0240 mL5 mM 0.5205 mL 2.6024 mL 5.2048 mL10 mM 0.2602

3、mL 1.3012 mL 2.6024 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Scopolamine hydrobromide親和的 (nM 級別) 毒蕈堿 (muscarinic) 拮抗劑。Scopolamine 可逆抑制 5-HT3 受體反應，IC50 為 2.09 M。1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50 & Target 5-HT3 Receptor mAChR2.09 M (IC50)體外研究 Application

4、 of Scopolamine to oocytes expressing 5-HT3 receptors does not elicit a response when appliedalone, but causes a concentration-dependent inhibition of the response during a co-application of 2 M 5-HT.The pIC50 value for Scopolamine is 5.680.05 (IC50=2.09 M, n=6) with a Hill Slope of 1.06 0.05. Thisg

5、ave a Kb of 3.23 M. The same concentration-dependent effect is also seen when Scopolamine is appliedduring the 5-HT application. To further test for a competitive binding at the 5-HT3 receptor, the competition ofunlabelled Scopolamine is measured with 3Hgranisetron, an established high-affinity comp

6、etitive antagonistat these receptors. Scopolamine displays concentration-dependent competition with 0.6 nM 3Hgranisetron(Kd), yielding an average pKi of 5.170.24 (Ki=6.76 M, n=3) 1.體內研究 In the histopathology study, there is no significant change in the histology of the brain. However, it isobserved

7、that there is a reduction in density of cells in the hippocampus of the control mice pretreated withScopolamine who received only distilled water 2. Scopolamine administration alone significantly increasesthe activity of Acetylcholinesterase enzyme (AchE) (7.980.065; P1-42) (P 3.PROTOCOLKinase Assay

8、 1 Saturation binding (8 point) curves are measured by incubating either crude extracts of HEK 293 cells stablyexpressing 5-HT3 receptors, or Guinea pig membrane preparations, in 0.5 mL incubations containing 10 mMHEPES buffer (pH 7.4) and 0.1-1 nM 3Hgranisetron or 1-10 nM 3HN-methylScopolamine. Com

9、petitionbinding (10 point) is determined by incubating the same receptors preparations in 0.5 mL HEPES buffercontaining either 0.6 nM 3Hgranisetron or 0.6 nM 3HN-methylScopolamine, and differing concentrations ofcompeting ligands. Non-specific binding is determined with 1 mM quipazine or 10 M Scopol

10、aminerespectively. Incubations are terminated by filtration onto Whatman GF/B filters wetted with HEPESbuffer+0.3% polyethyleneimine, followed by two rapid washes with ice-cold HEPES buffer. Proteinconcentration is calculated using a Lowry protein assay with bovine serum albumin standards. Radioacti

11、vityis measured using a Tri-Carb 2100 TR scintillation counter 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 23 The mice are weighed, labeled and grouped into seven groups of 5 animals each after which all animals arepre-

12、injected intraperitoneally with 3 mg/kg Scopolamine. Groups 1-3 are administered 0.2 mL equivalentdoses of 4 mg/kg, 6 mg/kg and 8 mg/kg of the extract of Morinda lucida while groups 4-6 are given samedoses of Peltophorum pterocarpum extract and group 7 is given 0.2 mL of distilled water (negative co

13、ntrol)for 3 consecutive days.Rats 3Healthy male Wistar rats (12 months old) weighing 180200 g are used in this study. Rats are divided intofive groups (n=6/group); Group I-normal control, Group II-disease control (Scopolamine hydrobromide 3mg/kg, i.p.), Group III-Scopolamine+Quercetin (25 mg/kg, p.o

14、.), Group IV-standard treatment(Scopolamine+Donepezil hydrochloride 3 mg/kg, p.o.), and Group V-Scopolamine+Quercetin (25 mg/kg,p.o.)+Donepezil (3 mg/kg, p.o.). Group III, IV, and V rats are dosed every 24 h interval with respective drugs2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEfor 14 consec

15、utive days. The acquisition trail for Morris water maze, elevated plus maze, and passiveavoidance paradigm is carried out on the 14th day, and Scopolamine (3 mg/kg, i.p.) is administered on the14th day after the acquisition trail to all groups except normal control group, which provoke the cognitive

16、impairment in rats. Retention of memory is tested on the 15th day, and on the same day, rats are sacrificedand brain tissues are isolated to estimate acetylcholinesterase enzyme (AchE) and brain oxidative stressmarkers such as lipid peroxidase (LPO), glutathione (GSH) (reduced). ELISA kit is used to

17、 estimate amyloid (A1-42) level. The hippocampus of rat brains is dissected out and studied for histopathologicalchanges.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Lochner M, et al. The muscarinic antagonists Scopolamine and atropine a

18、re competitive antagonists at 5-HT3 receptors.Neuropharmacology. 2016 Sep;108:220-8.2. O ET, et al. COGNITIVE-ENHANCING PROPERTIES OF MORINDA LUCIDA (RUBIACEAE) AND PELTOPHORUM PTEROCARPUM(FABACEAE) IN SCOPOLAMINE-INDUCED AMNESIC MICE. Afr J Tradit Complement Altern Med. 2017 Mar 1;14(3):136-141.3. Pattanashetti LA, et al. Evaluation of neuroprotective effect of Quercetin with Donepezil in Scop