A5736
ARC 239 二盐酸盐 水合物
≥98% (HPLC)
别名:
(2-[2-[4-(o-Methoxyphenyl)piperazin-1-yl]ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolinedione dihydrochloride hydrate
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关于此项目
经验公式（希尔记法）:
C24H29N3O3·2HCl · xH2O
化学文摘社编号:
分子量:
480.43 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
ARC 239 二盐酸盐 水合物, ≥98% (HPLC)
InChI key
KWVGFMWBNZTADI-UHFFFAOYSA-N
SMILES string
O.Cl.Cl.COc1ccccc1N2CCN(CC2)CCN3C(=O)c4ccccc4C(C)(C)C3=O
InChI
1S/C24H29N3O3.2ClH.H2O/c1-24(2)19-9-5-4-8-18(19)22(28)27(23(24)29)17-14-25-12-15-26(16-13-25)20-10-6-7-11-21(20)30-3;;;/h4-11H,12-17H2,1-3H3;2*1H;1H2
assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
H2O: >5 mg/mL
storage temp.
2-8°C
Quality Level
Application
ARC 239 is a potent α-adrenoceptor blocking drug, competitively antagonizing pressor responses to adrenaline and inhibiting pressor responses to noradrenaline, phenylephrine, tyramine, and dimethylphenylpiperazinium.
Biochem/physiol Actions
ARC 239 is a selective α-2B adrenergic blocker.
ARC 239 is a selective α-2B adrenergic blocker. Although ARC-239, like prazosin, also has some alpha-1 antagonist activity, it is used most commomly to differentiate alpha-2A/D from alpha-2B and alpha-2C subtypes rather than for any alpha-1 inhibition..
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
L Liu et al.
British journal of pharmacology, 120(5), 892-898 (1997-03-01)
1. The influence of the sympathetic nervous system on intestinal fluid transport by the jejunum and ileum of the anaesthetized rat was investigated under basal conditions and during active secretion induced by intra-arterial infusion of vasoactive intestinal peptide (VIP). 2.
R Colucci et al.
Neuroscience letters, 210(1), 29-32 (1996-05-24)
The effects of several alpha 2-adrenoceptor agonists and antagonists were examined on the cholinergic twitch contractions evoked by electrical field stimulation of guinea-pig duodenum. Oxymetazoline, xylazine, noradrenaline, alpha-methyl-noradrenaline or medetomidine (0.01-30 microM) were nearly equieffective in inhibiting duodenal twitch responses.
P Mouillé et al.
Journal of cardiovascular pharmacology, 2(2), 175-191 (1980-01-01)
In pentobarbital-treated dogs and rats, AR-C239, a new and potent alpha-adrenoceptor blocking drug, competitively antagonized pressor responses to adrenaline and inhibited pressor responses to noradrenaline, phenylephrine, tyramine, and dimethylphenylpiperazinium. Injected intravenously into closed-chest dogs, AR-C239 (3-50 micrograms/kg) induced a progressive
alpha2-Adrenoceptor-mediated potassium currents in acutely dissociated rat locus coeruleus neurones.
J Arima et al.
The Journal of physiology, 508 ( Pt 1), 57-66 (1998-06-06)
1. The noradrenaline (NA)-activated response was investigated in neurones acutely dissociated from the rat locus coeruleus (LC) using nystatin-perforated, conventional whole-cell and inside-out patch recording modes under current- and voltage-clamp conditions. 2. Under current-clamp conditions, NA hyperpolarized the LC neurones
S Esteban et al.
Naunyn-Schmiedeberg's archives of pharmacology, 353(4), 391-399 (1996-03-01)
The subtype determination of auto- and hetero-alpha 2-adrenoceptors modulating the synthesis of noradrenaline (NA) and serotonin (5-HT), respectively, was assessed using the accumulation of 3,4-dihydroxyphenylalanine (dopa) and 5-hydroxytryptophan (5-HTP) after decarboxylase inhibition as a measure of the rate of tyrosine
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