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Merck

SML0435

Sigma-Aldrich

AF-DX 116

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C24H31N5O2
CAS-Nummer:
Molekulargewicht:
421.54
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Arzneimittelkontrolle

regulated under CDSA - not available from Sigma-Aldrich Canada

Farbe

white to beige

Löslichkeit

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

Lagertemp.

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)

InChIKey

UBRKDAVQCKZSPO-UHFFFAOYSA-N

Anwendung

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. Wirkung

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.

Leistungsmerkmale und Vorteile

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.

Piktogramme

Exclamation mark

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Acute Tox. 4 Oral

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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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
S E McGowan
Respiratory physiology & neurobiology, 157(2-3), 281-289 (2007-02-27)
Vitamin A deficiency (VAD) remains an important problem in the developing world where environmental air pollution is increasing. Because the coincidence of these factors could increase the prevalence of asthma in these regions, airway reactivity to methacholine (MCh), capsaicin, and
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
Y Doi et al.
European journal of pharmacology, 505(1-3), 31-35 (2004-11-24)
This study characterized the functional effects of a novel gastroprokinetic agent, N-[2-(diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1, 3-thiazole-4-carboxyamide monohydrochloride trihydrate (Z338), on the muscarinic M1, M2, and M3 receptors expressed in Xenopus oocytes using the two-electrode voltage clamp method. Z-338 did not produce by itself
Leticia Ramírez-Lugo et al.
Neurobiology of learning and memory, 79(2), 184-193 (2003-02-20)
A number of studies have implicated cholinergic activity in the mediation of learning and memory processes. However, the specific role of muscarinic receptors in memory formation mechanisms is less known. The aim of the present study is to evaluate the

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