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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

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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
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
Jun Nomura et al.
Life sciences, 72(18-19), 2121-2126 (2003-03-12)
The existence and functions of muscarinic acetylcholine (mACh) receptors in human T lymphocytes were investigated. RT-PCR analysis demonstrated the presence of M(1) and M(2) subtypes of mACh receptors in human T lymphocytes. Pretreatment with oxotremorine-M (Oxo-M) caused the increase in
Julia B R Pfeiffer et al.
American journal of veterinary research, 68(3), 313-322 (2007-03-03)
To describe the in vitro effects of bethanechol on contractility of smooth muscle preparations from the small intestines of healthy cows and define the muscarinic receptor subtypes involved in mediating contraction. Tissue samples from the duodenum and jejunum collected immediately
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