(±)-Anatoxin A fumarate

Description: (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium. It acts as a potent nicotinic receptor agonist, exhibiting Ki values of 1.25 nM and 1.84 µM for binding to alpha4beta2-type nAChR and alpha7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [3H]-dopamine release from rat striatal synaptosomes with an EC50 of 134 nM. Target: Others. Smiles: OC(=O)\C=C\C(O)=O.CC(=O)C1=CCCC2CCC1N2. References: Tonn GR, Wong SG, Wong SC, et al. An inhibitory metabolite leads to dose- and time-dependent pharmacokinetics of (R)-N-{1-[3-(4-ethoxy-phenyl) -4-oxo-3,4-dihydro-pyrido[2,3-d]pyrimidin-2-yl]-ethyl}-N-pyridin-3-yl-methyl-2-(4-trifluoromethoxy-phenyl)-acetamide (AMG 487) in human subjects after multiple dosing. Drug Metabolism and Disposition, 2009, 37(3): 502-513.