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Submit ReviewAF-DX 116
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)
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.
| 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
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:
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
Gigout et al (2012) Distinct muscarinic acetylcholine receptor subtypes mediate pre- and postsynaptic effects in rat neocortex. BMC Neurosci 13 42 PMID: 22540185
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
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
Solanki et al (2007) Cholinergic innervation of the guinea-pig isolated vas deferens. Naunyn Schmiedebergs Arch Pharmacol 376 265 PMID: 17992517
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
Do you know of a great paper that uses AF-DX 116 from Tocris? Please let us know.
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