AF-DX 116

Name: AF-DX 116
Brand: Tocris Bioscience
SKU: 1105

Catalog # 1105 | Tocris Bioscience a Bio-Techne Brand

Citations (9)

COA / SDS

Selective M2 antagonist

Key Product Details

Description:	Selective M₂ antagonist
Alternative Names:	Otenzepad
Chemical Name:	11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Purity:	≥98% (HPLC)
Molecular Weight:	421.54

View Full Technical Details for AF-DX 116

Technical Data
Citations (9) / Reviews

Biological Activity for AF-DX 116

AF-DX 116 is a selective M₂ muscarinic receptor antagonist. K_i values are 64, 417, 786, 211 and 5130 nM for human recombinant M₂, M₁, M₃, M₄ and M₅ muscarinic receptors, respectively.

Licensing Information

Sold with the permission of Boehringer Ingelheim GmbH

Technical Data for AF-DX 116

M. Wt	421.54
Formula	C₂₄H₃₁N₅O₂
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	102394-31-0
PubChem ID	107867
InChi Key	UBRKDAVQCKZSPO-UHFFFAOYSA-N
Smiles	CCN(CC)CC1CCCCN1CC(=O)N1C2=C(C=CC=C2)C(=O)NC2=CC=CN=C12

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.

Solubility for AF-DX 116

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	10.54	25 with gentle warming

Preparing Stock Solutions for AF-DX 116

The following data is based on the product molecular weight 421.54.

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
0.25 mM	9.49 mL	47.45 mL	94.89 mL
1.25 mM	1.90 mL	9.49 mL	18.98 mL
2.5 mM	0.95 mL	4.74 mL	9.49 mL
12.5 mM	0.19 mL	0.95 mL	1.90 mL

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References for AF-DX 116

References are publications that support the biological activity of the product.

Mansfield Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing. Br.J.Pharmacol. 2005 PMID: 15723094
Eglen Muscarinic receptor subtypes and smooth muscle function. Pharmacol.Rev. 1996 PMID: 8981565
Billard 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. J.Pharmacol.Exp.Ther. 1995 PMID: 7714776
Hammer Binding profile of a novel cardioselective muscarinic receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat. Life Sci. 1986 PMID: 3754610

Citations for AF-DX 116 (9)

Showing 1 - 9 of 9 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for AF-DX 116 include:

Ross et al. (2019) Olfactory Bulb Muscarinic Acetylcholine Type 1 Receptors Are Required for Acquisition of Olfactory Fear Learning. Front Behav Neurosci. 13:164
PMID: 31379534
Bragança et al. (2016) Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria. Front Pharmacol. 7:45
PMID: 27014060
Bell et al. (2015) Acetylcholine release in mouse hippocampal CA1 preferentially activates inhibitory-selective interneurons via α4β2* nicotinic receptor activation. J Neurosci. 9:115
PMID: 25918499
Placeres-Uray et al. (2014) M2 Muscarinic acetylcholine receptor modulates rat airway smooth muscle cell proliferation. World Allergy Organ J. 6:22
PMID: 24377382
Gigout et al. (2012) Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex. BMC Neurosci. 13:42
PMID: 22540185
Kitazawa et al. (2009) M3 muscarinic receptors mediate positive inotropic responses in mouse atria: a study with muscarinic receptor knockout mice. Front Cell Neurosci. 330:487
PMID: 19429792
Clancy et al. (2007) Coregulation of natively expressed pertussis toxin-sensitive muscarinic receptors with G-protein-activated potassium channels. Proc Natl Acad Sci U S A. 27:6388
PMID: 17567799
Makara et al. (2007) Involvement of nitric oxide in depolarization-induced suppression of inhibition in hippocampal pyramidal cells during activation of cholinergic receptors. J Neurosci. 27:10211
PMID: 17881527
Solanki et al. (2007) Cholinergic innervation of the guinea-pig isolated vas deferens. Naunyn Schmiedebergs Arch Pharmacol. 376:265
PMID: 17992517

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