DMP 543

Biological Activity

DMP 543 is an acetylcholine release stimulator. Potently enhances K⁺-stimulated [³H]-ACh release from rat hippocampal slices (EC₅₀ = 700 nM), and 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. Also K⁺ channel blocker.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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.
   Zaczek et al.
   J.Pharmacol.Exp.Ther., 1998;285:724
2. 2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action.
   Earl et al.
   J.Med.Chem., 1998;41:4615

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