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SML0435

Sigma-Aldrich

AF-DX 116

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C24H31N5O2
Número CAS:
102394-31-0
Peso molecular:
421.54
Número MDL:
MFCD00864743
Código UNSPSC:
12352200
ID de substância PubChem:
329824718
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

powder

controle de medicamentos

regulated under CDSA - not available from Sigma-Aldrich Canada

cor

white to beige

solubilidade

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

temperatura de armazenamento

room temp

cadeia de caracteres SMILES

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)

chave InChI

UBRKDAVQCKZSPO-UHFFFAOYSA-N

Aplicação

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.

Ações bioquímicas/fisiológicas

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.

Características e benefícios

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.

Pictogramas

Exclamation mark
GHS07

Palavra indicadora

Warning

Frases de perigo

H302

Declarações de precaução

P264 - P270 - P301 + P312 - P501

Classificações de perigo

Acute Tox. 4 Oral

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

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Certificados de análise (COA)

Lot/Batch Number
082M4704V

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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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