Eseroline

Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine. 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].

469-22-7

12352005

H301-H311-H331

Cholinesterase (ChE) ; Drug Metabolite; nAChR; Opioid Receptor

GPCR/G Protein; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Neuroscience-Neurodegeneration

Neurological Disease

C[C@]12C3=CC(O)=CC=C3N([C@@]1([H])N(CC2)C)C

C13H18N2O

218.29

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P361+P364-P403+P233-P405-P501

[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. |[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.|[3]Somani SM, et al. Eseroline, a metabolite of physostigmine, induces neuronal cell death. Toxicol Appl Pharmacol. 1990 Oct;106 (1) :28-37.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W856819/

Reference compound1

No Development Reported

AChE; μ Opioid Receptor/MOR