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)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
方案
≥98% (HPLC)
表单
powder
颜色
white to off-white
溶解性
H2O: >5 mg/mL
储存温度
2-8°C
SMILES字符串
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
InChI key
KWVGFMWBNZTADI-UHFFFAOYSA-N
应用
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.
生化/生理作用
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..
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Aquatic Acute 1
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
I F Musgrave et al.
Biochemical pharmacology, 49(2), 187-196 (1995-01-18)
Human erythroleukaemia (HEL) cells were investigated to characterize their alpha 2-adrenoceptor and imidazoline receptor sites. Membranes from HEL cells bound [3H]2-(2-methoxy-1, 4-benzodioxan-2yl)-2-imidazoline ([3H]RX821002) in a saturable and specific manner with a KD of 0.64 +/- 0.07 nM and a Bmax
Y Mateo et al.
European journal of pharmacology, 379(1), 53-57 (1999-09-28)
The regulation of extracellular noradrenaline levels in the cingulate cortex by somatodendritic alpha2-adrenoceptors located in the locus coeruleus was evaluated in the rat by using dual-probe microdialysis. The concentration of noradrenaline in the cingulate cortex was decreased (37%-40%) by administration
L F Callado et al.
European journal of pharmacology, 366(1), 35-39 (1999-03-04)
In this study, we used subtype-selective antagonists to determine the subtype of alpha2-adrenoceptor controlling noradrenaline release in rat locus coeruleus. Noradrenaline release was measured in locus coeruleus slices using fast cyclic voltammetry at carbon fibre microelectrodes. On long stimulation trains
A Bencsics et al.
Brain research, 705(1-2), 302-306 (1995-12-24)
Exogenous pyrogens, e.g., bacterial lipopolysaccharides (LPS), are thought to stimulate macrophages to release endogenous pyrogens, e.g., TNF alpha, IL-1 beta, and IL-6, which act in the hypothalamus to produce fever. We studied the effect of different alpha 1- and alpha
M Taoda et al.
Neurochemistry international, 38(4), 317-322 (2001-01-04)
The presynaptic modulation of [3H]-noradrenaline (NA) release from rat kidney cortex slices, a method used for the first time, was investigated. Rat kidney cortex slices were loaded with [3H]-NA and the release of radioactivity at rest and in response to
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