AF-DX 116

Pricing Availability   Qty
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)
Datasheet
Citations (9)
Reviews
Literature (2)

Biological Activity for AF-DX 116

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.

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 Data for AF-DX 116

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 1.9 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 1.9 mL

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Product Datasheets for AF-DX 116

Certificate of Analysis / Product Datasheet
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References for AF-DX 116

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

Billard et al (1995) 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. 273 273 PMID: 7714776

Eglen et al (1996) Muscarinic receptor subtypes and smooth muscle function. Pharmacol.Rev. 48 531 PMID: 8981565

Hammer et al (1986) Binding profile of a novel cardioselective muscarinic receptor antagonist, AF-DX 116, to membranes of peripheral tissues and brain in the rat. Life Sci. 38 1653 PMID: 3754610

Mansfield et al (2005) Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing. Br.J.Pharmacol. 114 1089 PMID: 15723094


If you know of a relevant reference for AF-DX 116, please let us know.

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Keywords: AF-DX 116, AF-DX 116 supplier, Selective, M2, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, AFDX116, Otenzepad, 1105, Tocris Bioscience

9 Citations for AF-DX 116

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

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

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

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

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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