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Dihydro-β-erythroidine hydrobromide

现货
Catalog No.
B7030
nAChRs拮抗剂
组合的产品项目
规格价格库存 数量
10mg
¥ 4,240.00
Ship with 10-15 days

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Background

IC50: 1.3 μM for α2β2, 2.3 μM for α2β4, 0.41 μM for α3β2, 23.1 μM for α3β4, 0.37 μM for α4β2, and 0.19 μM for α4β4 [1]

Dihydro-β-erythroidine hydrobromide (DHβE), the hydrogenated derivative of erythroidine, is a competitive antagonist of neuronal nicotinic acetyicholine receptors (or nAChRs). Nicotinic acetyicholine receptors are neuron receptor proteins which respond to the neurotransmitter acetylcholine.

In vitro: DHβE has been shown to be a purely competitive antagonist of the neuronal nicotinic receptor [1].

In vivo: DHβE is able to block some of the central actions of nicotine after systemic and intrathecal administration. The mechanism of blockade is different from that of mecamylamine, a classical ganglionic antagonist, and may involve a direct action of DHβE on nicotine receptor [2].

Clinical trial: DHβE can be given orally and may cross the blood-brain barriers. At 200 mg/kg, the effects were bradycardia and visual difficulty most often described as blurring of vision or double vision; at 6 mg/kg, produced aforementioned effects plus hypotension and reduction in grip strength with accompanying feelings of sedation [3].

References:
[1] Harvey SC, Maddox FN, Luetje CW.  Multiple determinants of dihydro-beta-erythroidine sensitivity on rat neuronal nicotinic receptor alpha subunits. J Neurochem. 1996 Nov;67(5):1953-9.
[2] Damaj MI, Welch SP, Martin BR.  In vivo pharmacological effects of dihydro-beta-erythroidine, a nicotinic antagonist, in mice. Psychopharmacology (Berl). 1995 Jan;117(1):67-73.
[3] MURPHREE HB.  Effects in human volunteers of subparalytic doses of dihydro-beta-erythroidine. Clin Pharmacol Ther. 1963 May-Jun;4:304-10.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt356.26
Cas No.29734-68-7
FormulaC16H21NO3.HBr
Solubility<35.63mg/ml in H2O; <8.91mg/ml in DMSO
Chemical Name(2R,4aS,7R,13bS)-2-methoxy-12-oxo-2,4a,5,6,7,8,9,10,12,13-decahydro-1H-pyrano[4',3':3,4]pyrido[2,1-i]indol-7-ium bromide
SDFDownload SDF
Canonical SMILESO=C1OCC2=C(C1)[C@@]3(C4)[N@@H+](CC2)CC[C@H]3C=C[C@@H]4OC.[Br-]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

非洲爪蟾卵母细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

300nM或1 μM

实验结果

在浓度为1 μM时,Dihydro-β-erythroidine Hydrobromide几乎完全阻断α4β4亚基,但对α3β4亚基几乎没有影响。然而,Dihydro-β-erythroidine Hydrobromide对α4β4亚基的阻断作用可以通过增加激动剂浓度来逆转。在300 nM Dihydro-β-erythroidine Hydrobromide存在的情况下,表达α4β4的卵母细胞对5 μM和500 μM ACh的电流响应分别为Ach单独引起电流响应的36.0 ± 9.0 %和97.1 ± 9.6 %。

动物实验 [2]:

动物模型

尼古丁诱导的低温小鼠模型

给药剂量

0、1.8、3.6、7.2或10.8 μmol/kg;皮下注射

实验结果

在尼古丁诱导的低温小鼠模型中,Dihydro-β-erythroidine Hydrobromide呈剂量依赖性地缓解低温,其AD50值为6.2 μmol/kg。然而,在上述剂量下,Dihydro-β-erythroidine Hydrobromide对非尼古丁诱导的体温升高无显著影响。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Harvey SC, Maddox FN, Luetje CW. Multiple determinants of dihydro-beta-erythroidine sensitivity on rat neuronal nicotinic receptor alpha subunits. J Neurochem. 1996 Nov;67(5):1953-9.

[2]. Damaj MI, Welch SP, Martin BR. In vivo pharmacological effects of dihydro-beta-erythroidine, a nicotinic antagonist, in mice. Psychopharmacology (Berl). 1995 Jan;117(1):67-73.

质量控制

质量控制和MSDS

批次:

化学结构

Dihydro-β-erythroidine hydrobromide