Galanthamine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

人 nAChR α4β2、α3β4 和 α6β4 的有效变构增强配体；在 0.1-1 uM 时增强四种 nAChR 亚型的激动剂反应。

A potent allosteric potentiating ligand of human nAChRs α4β2, α3β4, and α6β4; potentiates agonist responses of the four nAChR subtypes at 0.1-1 uM, acts as an nAChR inhibitor at >10 uM; also shows affinity for chicken/mouse nAChRs α7/5-HT3 in certain areas of the brain; also works as a weak competitive and reversible cholinesterase inhibitor with IC50 of 2.8-3.2 uM; decreases genotoxicity and cell death induced by β-amyloid peptide in SH-SY5Y cell line.Alzheimer's Disease Approved(In Vitro):Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes. (In Vivo):Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine.

Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes.

Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine.

NSC 100058

Membrane Transporter/Ion Channel

nAChR

nAChR

Neurological Disease

Alzheimer Disease

357-70-0

287.3535

C17H21NO3

>98% (HPLC)

DMSO: ≥ 59 mg/mL

O[C@H]1C=C[C@@]23CCN(C)CC4=CC=C(OC)C(O[C@@]3([H])C1)=C24

6H-Benzofuro[3a,3,2-ef][2]benzazepin-6-ol, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-, (4aS,6R,8aS)-

(-20℃)

With Ice Pack

≥ 2 years