AF-DX 116

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Cat.No. 1105 - AF-DX 116 | C24H31N5O2 | CAS No. 102394-31-0
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 (4)
Literature

Biological Activity

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

Compound Libraries

AF-DX 116 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 421.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.37 mL 11.86 mL 23.72 mL
5 mM 0.47 mL 2.37 mL 4.74 mL
10 mM 0.24 mL 1.19 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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

4 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

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

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? If so please let us know.

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