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SML0435

Sigma-Aldrich

AF-DX 116

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C24H31N5O2
CAS Number:
102394-31-0
Molecular Weight:
421.54
MDL number:
MFCD00864743
UNSPSC Code:
12352200
PubChem Substance ID:
329824718
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

drug control

regulated under CDSA - not available from Sigma-Aldrich Canada

color

white to beige

solubility

DMSO: 5 mg/mL (clear solution; warmed)

storage temp.

room temp

SMILES string

CCN(CC)CC1CCCCN1CC(=O)N2c3ccccc3C(=O)Nc4cccnc24

InChI

1S/C24H31N5O2/c1-3-27(4-2)16-18-10-7-8-15-28(18)17-22(30)29-21-13-6-5-11-19(21)24(31)26-20-12-9-14-25-23(20)29/h5-6,9,11-14,18H,3-4,7-8,10,15-17H2,1-2H3,(H,26,31)

InChI key

UBRKDAVQCKZSPO-UHFFFAOYSA-N

Application

AF-DX 116 has been used as an M2 muscarinic acetylcholine receptor (M2AChR) selective antagonist to study the influence of M2AChR in the regulation of both basal and carbachol-stimulated long-term potentiation at the dentate gyrus (DG-LTP) and pro-nerve growth factor (proNGF) secretion in hippocampal cells of young diabetic rats.

Biochem/physiol Actions

AF-DX 116 is a selective M2 muscarinic acetylcholine receptor antagonist.
AF-DX 116 raises blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress. Thus, it may be used as a therapeutic for hypotension related to vagotonia type autonomic dysfunction.

Features and Benefits

This compound is featured on the Acetylcholine Receptors (Muscarinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000136155
0000136211
0000083332
0000033489
0000033490

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M Marti et al.
Journal of veterinary pharmacology and therapeutics, 28(6), 565-574 (2005-12-14)
The goal of this study was to investigate the effect of bethanechol (BeCh) on contractility patterns of smooth muscle preparations of equine duodenum descendens, jejunum, caecum and pelvic flexure in vitro. Concentration-response relationships were developed for BeCh using in vitro
Eugeny E Nikolsky et al.
The Journal of physiology, 560(Pt 1), 77-88 (2004-07-16)
The effects of cholinergic drugs on the quantal contents of the nerve-evoked endplate currents (EPCs) and the parameters of the time course of quantal release (minimal synaptic latency, main modal value of latency histogram and variability of synaptic latencies) were
S Gigout et al.
Neuroscience, 223, 399-411 (2012-08-07)
Acetylcholine has been implicated in higher cortical functions such as learning, memory and cognition, yet the cellular effects of muscarinic acetylcholine receptor (mAChR) activation are poorly understood in the human cortex. Here we investigated the effect of the mAChR agonist
Marzia Soligo et al.
Scientific reports, 7(1), 9077-9077 (2017-08-24)
The muscarinic receptor response to acetylcholine regulates the hippocampal-related learning, memory, neural plasticity and the production and processing of the pro-nerve growth factor (proNGF) by hippocampal cells. The development and progression of diabetes generate a mild cognitive impairment reducing the
Takio Kitazawa et al.
European journal of pharmacology, 554(2-3), 212-222 (2006-11-23)
Functional roles of muscarinic acetylcholine receptors in the regulation of mouse stomach motility were examined using mice genetically lacking muscarinic M(2) receptor and/or M(3) receptor and their corresponding wild-type (WT) mice. Single application of carbachol (1 nM-30 microM) produced concentration-dependent
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