AF-DX 116
Chemical Name: 11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Purity: ≥98%
Biological Activity
AF-DX 116 is a selective M2 muscarinic receptor antagonist. Ki values are 64, 417, 786, 211 and 5130 nM for human recombinant M2, M1, M3, M4 and M5 muscarinic receptors, respectively.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.
Additional Information
Background References
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Autoimmunity against M(2)muscarinic acetylcholine receptor induces myocarditis and leads to a dilated cardiomyopathy-like phenotype.
Yoshizawa A, Nagai S, Baba Y, Yamada T, Matsui M, Tanaka H, Miyoshi S, Amagai M, Yoshikawa T, Fukuda K, Ogawa S, Koyasu S
Eur. J. Immunol., 2012;42(5):1152-63. -
High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Identification of the primary muscarinic autoreceptor subtype in rat striatum as M2 through a correlation of in vivo microdialysis and in vitro receptor binding data.
Billard et al.
J.Pharmacol.Exp.Ther., 1995;273:273 -
Muscarinic receptor subtypes and smooth muscle function.
Eglen et al.
Pharmacol.Rev., 1996;48:531 -
Binding profile of a novel cardioselective muscarinic receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat.
Hammer et al.
Life Sci., 1986;38:1653 -
Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing.
Mansfield et al.
Br.J.Pharmacol., 2005;114:1089
Product Datasheets
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Citations for AF-DX 116
The citations listed below are publications that use Tocris products. Selected citations for AF-DX 116 include:
9 Citations: Showing 1 - 9
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Olfactory Bulb Muscarinic Acetylcholine Type 1 Receptors Are Required for Acquisition of Olfactory Fear Learning.
Authors: Ross Et al.
Front Behav Neurosci 2019;13:164
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Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria.
Authors: Bragança Et al.
Front Pharmacol 2016;7:45
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Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation.
Authors: Bell Et al.
J Neurosci 2015;9:115
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M2 Muscarinic acetylcholine receptor modulates rat airway smooth muscle cell proliferation.
Authors: Placeres-Uray Et al.
World Allergy Organ J 2014;6:22
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Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex.
Authors: Gigout Et al.
BMC Neurosci 2012;13:42
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M3 muscarinic receptors mediate positive inotropic responses in mouse atria: a study with muscarinic receptor knockout mice.
Authors: Kitazawa Et al.
Front Cell Neurosci 2009;330:487
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Cholinergic innervation of the guinea-pig isolated vas deferens.
Authors: Solanki Et al.
Naunyn Schmiedebergs Arch Pharmacol 2007;376:265
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Coregulation of natively expressed pertussis toxin-sensitive muscarinic receptors with G-protein-activated potassium channels.
Authors: Clancy Et al.
Proc Natl Acad Sci U S A 2007;27:6388
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Involvement of nitric oxide in depolarization-induced suppression of inhibition in hippocampal pyramidal cells during activation of cholinergic receptors.
Authors: Makara Et al.
J Neurosci 2007;27:10211
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