457075-21-7
Chemical Structure
Ganstigmine
Synonym(s): CHF 2819 free base
- CAS No.: 457075-21-7
- Formula:C22H27N3O3
- Molecular Weight:381.47
InChIKey: ZOBDWFRKFSPCRB-UNMCSNQZSA-N
SMILES: C[C@]12C3=CC(OC(NC4=C(C=CC=C4)CC)=O)=CC=C3N([C@@]1([H])ON(CC2)C)C
Biological Activity: Ganstigmine (CHF 2819 free base) is a potent, orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor, with an IC50 value of 65 nM against human AChE, 310 nM against human butyrylcholinesterase (BChE), and 5.12 μM against Torpedo californica AChE. Ganstigmine increases extracellular acetylcholine levels in the brain of rodents without altering the concentrations of other neurotransmitters, stimulates cholinergic transmission, and induces the release of soluble non-amyloidogenic amyloid precursor protein. Ganstigmine exhibits neuroprotective activity independent of cholinesterase inhibition, prevents neuronal death, alleviates β-amyloid-induced neurodegeneration, rescues cholinergic neuron loss, and reverses Scopolamine (HY-N0296)-induced amnesia and memory deficits. Ganstigmine shows cholinesterase inhibition-independent neuroprotective effects against growth factor deprivation and Aβ25-35 toxicity. Ganstigmine can be used in research on Alzheimer's disease, cholinergic dysfunction, and neuroprotection[1][2][3][4][5].
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Ganstigmine | Ganstigmine (CHF 2819 free base) is a potent, orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor, with an IC50 value of 65 nM against human AChE, 310 nM against human butyrylcholinesterase (BChE), and 5.12 μM against Torpedo californica AChE. Ganstigmine increases extracellular acetylcholine levels in the brain of rodents without altering the concentrations of other neurotransmitters, stimulates cholinergic transmission, and induces the release of soluble non-amyloidogenic amyloid precursor protein. Ganstigmine exhibits neuroprotective activity independent of cholinesterase inhibition, prevents neuronal death, alleviates β-amyloid-induced neurodegeneration, rescues cholinergic neuron loss, and reverses Scopolamine (HY-N0296)-induced amnesia and memory deficits. Ganstigmine shows cholinesterase inhibition-independent neuroprotective effects against growth factor deprivation and Aβ25-35 toxicity. Ganstigmine can be used in research on Alzheimer's disease, cholinergic dysfunction, and neuroprotection. | |||||||||||||||||||||
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- [1]. Bartolucci C, et al. Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819). Journal of medicinal chemistry. 2006 Aug 24;49(17):5051-8. [Content Brief]
- [2]. Yu QS, et al. Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. Journal of medicinal chemistry. 2002 Aug 15;45(17):3684-91. [Content Brief]
- [3]. Windisch M et al. The protective effect of ganstigmine against amyloid beta 25-35 neurotoxicity on chicken cortical neurons is independent from the cholinesterase inhibition. Neurosci Lett. 2003 May 8;341(3):181-4. [Content Brief]
- [4]. Capsoni S et al. Ganstigmine and donepezil improve neurodegeneration in AD11 antinerve growth factor transgenic mice. Am J Alzheimers Dis Other Demen. 2004 May-Jun;19(3):153-60. [Content Brief]
- [5]. Trabace L et al. Neurochemical and neurobehavioral effects of ganstigmine (CHF2819), a novel acetylcholinesterase inhibitor, in rat prefrontal cortex: an in vivo study. Pharmacol Res. 2007 Oct;56(4):288-94. [Content Brief]
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