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Scopolamine

CAS No. : 51-34-3

MCE 站：Scopolamine

产品活性：Scopolamine 是高亲和力的 (nM 级别) 毒蕈碱 (muscarinic) 拮抗剂。Scopolamine 可逆抑制 5-HT₃ 受体反应，IC₅₀ 为 2.09 μM。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease

作用靶点：mAChR  |  5-HT Receptor  |  Endogenous Metabolite

In Vitro: Application of Scopolamine to oocytes expressing 5-HT₃ receptors does not elicit a response when applied alone, but causes a concentration-dependent inhibition of the response during a co-application of 2 μM 5-HT. The pIC₅₀ value for Scopolamine is 5.68±0.05 (IC₅₀=2.09 μM, n=6) with a Hill Slope of 1.06 ± 0.05. This gave a K_b of 3.23 μM. The same concentration-dependent effect is also seen when Scopolamine is applied during the 5-HT application. To further test for a competitive binding at the 5-HT₃ receptor, the competition of unlabelled Scopolamine is measured with [³H]granisetron, an established high-affinity competitive antagonist at these receptors. Scopolamine displays concentration-dependent competition with 0.6 nM [³H]granisetron (~K_d), yielding an average pK_i of 5.17±0.24 (K_i=6.76 μM, n=3).

In Vivo: In the histopathology study, there is no significant change in the histology of the brain. However, it is observed that there is a reduction in density of cells in the hippocampus of the control mice pretreated with Scopolamine who received only distilled water. Scopolamine administration alone significantly increases the activity of Acetylcholinesterase enzyme (AchE) (7.98±0.065; P<0.001) when compared to the normal group (3.06±0.296). The animals treated with Scopolamine report a significant increase (34.61±4.85; P<0.01) in levels of malondialdehyde (MDA) as compared to the normal group (12.82±2.86). The Scopolamine-treated group shows significant decrease in reduced glutathione (GSH) level (P<0.001; 0.1504±0.03) as compared to the normal group (0.3906±0.02). The Scopolamine-treated rats show a significant increase in the concentration ofβ amyloid (Aβ_1-42) (P<0.001; 146.2±1.74) as compared to the normal group (43.21±3.46).

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