产品
编 号:F546727
分子式:C17H22BrNO3
分子量:368.27
产品类型
结构图
CAS No: 1953-04-4
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生物活性:
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
体内研究:
Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p. ) reduces cognitive deficits in APP23 mice.Galanthamine hydrobromide (10 mg/kg; i.g.) displays short elimination half-life of approximately 2 h in wild-type mice.Animal Model:APP23 mice
Dosage:1.25 mg/kg, 2.5 mg/kg
Administration:Intraperitoneal injection, daily, 1 week
Result:Effectively remedied the spatial learning deficit.
Animal Model:Female 57B1/6J wild type
Dosage:10 mg/kg
Administration:Oral gavage (Pharmacokinetic Analysis)
Result:Cmax (0.31 μg/mL), t1/2β (1.6 h), AUC0-24h (0.67 μg ? h/mL).
体外研究:
Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase.Galanthamine hydrobromide (25-1000 μM) inhibits both Aβ 1-40 (50 μM) and Aβ 1-42 (50 μM) aggregation.Galanthamine hydrobromide (25-1000 μM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells.Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis.