1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEScopolamineCat. No.: HY-N0296CAS No.: 51-34-3Synonyms: Hyoscine; Scopine (-)-tropate; Scopine tropate分式: CHNO分量: 303.35作靶點: mAChR; 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Please store the product under the recom

2、mended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Scopolamine親和的 (nM 級別) 毒蕈堿 (muscarinic) 拮抗劑。Scopolamine 可逆抑制 5-HT3 受體反應(yīng)，IC50 為 2.09 M。IC50 & Target 5-HT3 Receptor mAChR2.09 M (IC50)體外研究 Application of Scopolamine to oocytes expressing 5-HT3 receptors does not elicit a response when appliedalone,

3、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. Thisgave a Kb of 3.23 M. The same concentration-dependent effect is also seen when Scopolamine is applied

4、during 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 competitive antagonistat these receptors. Scopolamine displays concentration-dependent competition with

5、0.6 nM 3Hgranisetron(Kd), yielding an average pKi of 5.170.24 (Ki=6.76 M, n=3) 1.體內(nèi)研究 In the histopathology study, there is no significant change in the histology of the brain. However, it isobserved that there is a reduction in density of cells in the hippocampus of the control mice pretreated with

6、Scopolamine who received only distilled water 2. Scopolamine administration alone significantly increasesthe activity of Acetylcholinesterase enzyme (AchE) (7.980.065; P1-42) (P 3.PROTOCOL1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEKinase Assay 1 Saturation binding (8 point) curves are measured

7、 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. Competitionbinding (10 point) is determined by incubat

8、ing 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 Scopolaminerespectively. Incubations are terminated by fi

9、ltration 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. Radioactivity ismeasured using a Tri-Carb 2100 TR scintillat

10、ion 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-injected intraperitoneally with 3 mg/kg Scopolamine

11、. 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 control) for3 consecutive days.Rats 3Healthy male Wis

12、tar rats (12 months old) weighing 180200 g are used in this study. Rats are divided into fivegroups (n=6/group); Group I-normal control, Group II-disease control (Scopolamine hydrobromide 3 mg/kg,i.p.), Group III-Scopolamine+Quercetin (25 mg/kg, p.o.), Group IV-standard treatment(Scopolamine+Donepez

13、il 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 drugsfor 14 consecutive days. The acquisition trail for Morris water maze, elevated plus maze, and passiveavoidance pa

14、radigm 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 cognitiveimpairment in rats. Retention of memory is tested on the 15th day, and on the same day, rats are sac

15、rificedand 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 estimate amyloid(A1-42) level. The hippocampus of rat brains is dissected out and studied for histo

16、pathological changes.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 are competitive antagonists at 5-HT3 receptors.Neuropharmacology. 2016 Sep;108:220-8.2. O ET, et al.

17、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 Scopolamine-induced amnesia in rats. IndianJ Pharmacol. 2017 Jan-Feb;49