Dihydro-β-erythroidine hydrobromide
(Synonyms: DHβE hydrobromide) 目录号 : GC13118
Dihydro-β-erythroidine (DHβE) hydrobromide 是一种有效的、具有口服活性的竞争性神经元 nAChR 拮抗剂。
Cas No.:29734-68-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Xenopus oocytes |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
300nM or 1 μM |
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Applications |
At the concentration of 1 μM, Dihydro-β-erythroidine Hydrobromide almost completely blocked the α4β4 subunit but showed little effect on the α3β4 subunit. However, the blockade effect of Dihydro-β-erythroidine Hydrobromide on the α4β4 subunit could be reversed by increasing the agonist concentration. In the presence of 300 nM Dihydro-β-erythroidine Hydrobromide, the current response of α4β4-expressing oocytes to 5 μM and 500 μM ACh were 36.0 ± 9.0 % and 97.1 ± 9.6 % of the response to ACh alone, respectively. |
| Animal experiment [2]: | |
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Animal models |
A nicotine-induced hypothermia mouse model |
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Dosage form |
0, 1.8, 3.6, 7.2 or 10.8 μmol/kg; s.c. |
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Applications |
In a nicotine-induced hypothermia mouse model, Dihydro-β-erythroidine Hydrobromide dose-dependently attenuated hypothermia, with the AD50 value of 6.2 μmol/kg. But it did not have a significant effect on the non-nicotine-induced increase in body temperature at the inducated doses. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 29734-68-7 | SDF | |
| 别名 | DHβE hydrobromide | ||
| 化学名 | (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 | ||
| Canonical SMILES | O=C1OCC2=C(C1)[C@@]3(C4)[N@@H+](CC2)CC[C@H]3C=C[C@@H]4OC.[Br-] | ||
| 分子式 | C16H21NO3.HBr | 分子量 | 356.26 |
| 溶解度 | <35.63mg/ml in Water; <8.91mg/ml in DMSO | 储存条件 | 4°C, sealed storage, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8069 mL | 14.0347 mL | 28.0694 mL |
| 5 mM | 0.5614 mL | 2.8069 mL | 5.6139 mL |
| 10 mM | 0.2807 mL | 1.4035 mL | 2.8069 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet