Cat. No. 2330
Chemical Name: 10,10-bis[(2-Fluoro-4-pyridinyl)met
Biological ActivityK+ channel blocker and acetylcholine release stimulator. Potently enhances K+-stimulated [3H]-ACh release from rat hippocampal slices (EC50 = 700 nM), and also increases release of dopamine and glutamate (EC50 values are 0.25 and 0.22 μM, respectively). Orally active in vivo; increases ACh levels in rats (with a minimum effective dose of 1 mg/kg) and exerts a long duration of action. More potent than linopirdine (Cat. No. 1999) both in vitro and in vivo.
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Certificate of Analysis / Product Datasheet / Safety Data Sheet
Earl et al (1998) 2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action. J.Med.Chem. 41 4615. PMID: 9804701.
Zaczek et al (1998) Two new potent neurotransmitter release enhancers, 10,10-Bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-Bis(2-fluoro-4-pyridinylmethyl)-9(10H)-anthracenone: comparison to linopirdine. J.Pharmacol.Exp.Ther. 285 724. PMID: 9580619.
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