Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
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.
View Related Products by Target
View Related Products by Product Action
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
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
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
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
Do you know of a great paper that uses AF-DX 116 from Tocris? Please let us know.
Reviews for AF-DX 116
There are currently no reviews for this product. Be the first to review AF-DX 116 and earn rewards!
Have you used AF-DX 116?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GPCR Product Listing
A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:
- Rhodopsin-like Receptors
- Glutamate Receptors
- Frizzled Receptors
- GPCR Signaling
Alzheimer's Disease PosterNew
Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.
Cardiovascular Poster
Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Schizophrenia Poster
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.