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Orthosteric neuronal nicotinic acetylcholine receptor (nAChR) antagonist (IC50 values are 0.17, 0.25, 0.4, 4.8, 6.5, 8.2, 20 and 34 μM at α3β4, α1β1εδ, α3β4β3, α6β4β3, α7, α4β2, α3β2β3 and α6/3β2β3 receptors respectively). Attenuates nicotine-evoked dopamine release from the ventral tegmental area in vivo (IC50 = 0.2 nM) and reduces nicotine self-administration in rats. Brain penetrant.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 514.38. Batch specific molecular weights may vary from batch to batch due to the degree 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||1.94 mL||9.72 mL||19.44 mL|
|5 mM||0.39 mL||1.94 mL||3.89 mL|
|10 mM||0.19 mL||0.97 mL||1.94 mL|
|50 mM||0.04 mL||0.19 mL||0.39 mL|
References are publications that support the biological activity of the product.
Dwoskin et al (2008) N,N'alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: Inhibition of nicotine-evoked DA release and hyperactivity. J.Pharmacol.Exp.Ther. 326 563 PMID: 18460644
Rahman et al (2008) Region-specific effects of the N,N'-dodecane-1,12-diyl-bis-3-picolinium dibromide on nicotine-induced increase in extracellular DA in vivo. Br.J.Pharmacol. 153 792 PMID: 18059317
Ayers et al (2002) Bis-azaaromatic quaternary ammonium analogues: ligands for α4β2* and β7* subtypes of neuronal nicotinic receptors Bioorg.Med.Chem.Letts. 12 3067
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Keywords: bPiDDB, bPiDDB supplier, bPiDDB, nicotinic, acetylcholine, receptors, nachrs, orthosteric, antagonists, a3b4, alpha3beta4, α3β4, brain, penetrant, Nicotinic, Receptors, (Non-selective), 3221, Tocris Bioscience
1 Citation for bPiDDB
Citations are publications that use Tocris products. Selected citations for bPiDDB include:
Holt et al (2015) Pharmacologically distinct nicotinic acetylcholine receptors drive efferent-mediated excitation in calyx-bearing vestibular afferents. J Cell Biol 35 3625 PMID: 25716861
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Literature in this Area
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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.