Bioactivity | 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)[1][2][3]. |
Target | IC50: 0.35 µM (AChE) |
Invitro | Galanthamine hydrobromide is 53-fold selectivity for AChE over butyrylcholinesterase[2].Galanthamine hydrobromide (25-1000 µM) inhibits both Aβ 1-40 (50 µM) and Aβ 1-42 (50 µM) aggregation[4].Galanthamine hydrobromide (25-1000 µM) protects against Aβ(1-40) and Aβ(1-42) toxicity in SH-SY5Y cells[4].Galanthamine hydrobromide also dramatically reduces Aβ(1-40)-induced cellular apoptosis[4]. |
In Vivo | Galanthamine hydrobromide (1.25-2.5 mg/kg; i.p. ) reduces cognitive deficits in APP23 mice[5].Galanthamine hydrobromide (10 mg/kg; i.g.) displays short elimination half-life of approximately 2 h in wild-type mice[6]. Animal Model: |
Name | Galanthamine hydrobromide |
CAS | 1953-04-4 |
Formula | C17H22BrNO3 |
Molar Mass | 368.27 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. L J Scott, et al. Galantamine: a review of its use in Alzheimer's disease. Drugs. 2000 Nov;60(5):1095-122. [2]. Marek Samochocki, et al. Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors. Pharmacol Exp Ther. 2003 Jun;305(3):1024-36. [3]. Acharya Balkrishna, et al. Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study. Molecules. 2019 Nov; 24(22): 4175. [4]. Balpreet Matharu, et al. Galantamine inhibits beta-amyloid aggregation and cytotoxicity. J Neurol Sci. 2009 May 15;280(1-2):49-58. [5]. Debby Van Dam, et al. Symptomatic effect of donepezil, rivastigmine, galantamine and memantine on cognitive deficits in the APP23 model. Psychopharmacology (Berl). 2005 Jun;180(1):177-90. [6]. Johan Monbaliu, et al. Pharmacokinetics of galantamine, a cholinesterase inhibitor, in several animal species. Arzneimittelforschung. 2003;53(7):486-95. |