K+ 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.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 412.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.42 mL||12.12 mL||24.25 mL|
|5 mM||0.48 mL||2.42 mL||4.85 mL|
|10 mM||0.24 mL||1.21 mL||2.42 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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
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
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Keywords: K+ channels blockers potent ACh release enhancer Potent orally active Potassium Channels Non-Selective Acetylcholine Nicotinic Receptors nAChR Muscarinic DMP543 Two-P Potassium Channels
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Literature in this Area
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.