AF-DX 116

Cat. No. 1105

AF-DX 116 C24H31N5O2 [102394-31-0]

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Alternative Name: Otenzepad

Chemical Name: 11-[[2-[(Diethylamino)methyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

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

Technical Data

M.Wt:
421.54
Formula:
C24H31N5O2
Solubility:
Soluble to 25 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
102394-31-0

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

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.

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

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.

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.

If you know of a relevant reference for this product please let us know.

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

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.

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.

Do you know of a great paper that uses AF-DX 116 from Tocris? If so please let us know.show all ▼show less ▲

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

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