Cat. No. 3221
Chemical Name: 1,1'-(1,12-Dodecanediyl)bis[3-methyl
Biological ActivityOrthosteric 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Dwoskin et al (2008) N,N'alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: Inhibition of nicotine-evoked dopamine 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 dopamine 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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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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Keywords: bPiDDB, supplier, bPiDDB, nicotinic, acetylcholine, receptors, nachrs, orthosteric, antagonists, a3b4, alpha3beta4, α3β4, brain, penetrant, Tocris Bioscience, Nicotinic Receptor (Non-selective) Antagonist products
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Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
August 20 - 24, 2017
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