469-22-7
Chemical Structure
Eseroline
- CAS No.: 469-22-7
- Formula:C13H18N2O
- Molecular Weight:218.29
InChIKey: HKGWQUVGHPDEBZ-OLZOCXBDSA-N
SMILES: C[C@]12C3=CC(O)=CC=C3N([C@@]1([H])N(CC2)C)C
Biological Activity: Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease[1][2][3].
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Eseroline | Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Motel WC, et al. Cholinergic modulation by opioid receptor ligands: potential application to Alzheimer's disease. Mini Rev Med Chem. 2013 Mar;13(3):456-66. [Content Brief]
- [2]. Galli A, et al. Reversible inhibition of acetylcholinesterase by eseroline, an opioid agonist structurally related to physostigmine (eserine) and morphine. Biochem Pharmacol. 1982 Apr 1;31(7):1233-8. [Content Brief]
- [3]. Somani SM, et al. Eseroline, a metabolite of physostigmine, induces neuronal cell death. Toxicol Appl Pharmacol. 1990 Oct;106(1):28-37. [Content Brief]
Keywords
