nAChR agonist 1 是一种有效的、脑通透性强的、口服有效的 α7 烟碱乙酰胆碱受体 (α7 nicotinic acetylcholine receptor) 的正向变构调节剂。nAChR agonist 1 在 Ca²⁺ 中，对内源性表达 α7 nAChR 的人 IMR-32 神经母细胞瘤细胞的 EC₅₀ 为 0.32 μM。nAChR agonist 1 可用于阿尔茨海默病的研究。

nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC 50 of 0.32 μM in a Ca mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.

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Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial.
nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.
nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T 1/2 , CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Sinha N, et al.Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relati

In Vitro: DMSO : 125 mg/mL (297.66 mM; Need ultrasonic)配制储备液