Idazoxan hydrochloride
(Synonyms: 盐酸咪唑克生) 目录号 : GC15813
盐酸咪唑克生（Idazoxan hydrochloride ，RX 781094 hydrochloride ，IDA）是一种分子量为241的α2-肾上腺和咪唑啉受体配体。
Cas No.:79944-56-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment [1]: |
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Cell lines |
C6 glioma cells |
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Preparation method |
Incubation of the C6 cells with 10 μM idazoxan for 5 days |
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Reaction Conditions |
10 μM；5 days |
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Applications |
in vitro resulted in a 23% reduction of β-adrenoceptor number and a 37% decrease in isoproterenol-induced cyclic AMP accumulation. |
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Animal experiment [2]: |
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Animal models |
SNL6W rats |
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Preparation method |
7,8-DHF (5 mg/kg/d) with or without ANA-12 (0.5 mg/kg/d) was injected intraperitoneally for 5 days from day 37 to 41 after the SNL surgery. K252a was dissolved in saline containing 10% DMSO. K252a (2 µg/10 µL) was administrated through an intrathecal catheter at a volume of 10 µL and then flushed with saline (10 µL) just before the intraperitoneal injection of 7,8-DHF. Idazoxan hydrochloride, propranolol, and atropine were dissolved in saline. Idazoxan (30 µg/10 µL), propranolol (30 µg/10 µL), or atropine (30 µg/10 µL) were administrated through an intrathecal catheter as described above 15 minutes before the capsaicin injection. |
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Dosage form |
30 µg/10 µ L |
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Applications |
Idazoxan blocked the 7,8-DHF–induced enhancement of NSIA in SNL6W rats (P < .001). |
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References: [1]. Manji H K , Chen G , Bitran J A ,et al.Idazoxan down-regulates beta-adrenoceptors on C6 glioma cells in vitro.[J].European Journal of Pharmacology Molecular Pharmacology, 1992, 227(3):275-282. [2]. Kato D , Suto T , Obata H ,et al.Spinal Activation of Tropomyosin Receptor Kinase-B Recovers the Impaired Endogenous Analgesia in Neuropathic Pain Rats.[J].Anesth Analg, 2019(2). |
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Idazoxan hydrochloride (RX 781094 hydrochloride, IDA) is a ligand for α2-adrenergic and imidazoline receptors with a molecular weight of 241. It binds to mitochondrial membranes and promotes apoptosis in pancreatic β cells[1]. Additionally, it competitively antagonizes the central hypotensive effects of imidazoline-like active molecules (IMs) [2]. It's worth noting that Idazoxan hydrochloride has been reported to improve motor symptoms in Parkinson's disease, levodopa-induced motor disturbances, and experimental Parkinson's syndrome.
In vitro studies demonstrate that incubating rat glioma C6 cells with 10 μM Idazoxan hydrochloride for 5 days leads to a 23% reduction in β-adrenergic receptor numbers and a 37% decrease in isoproterenol-induced cAMP accumulation[5]. Furthermore, Idazoxan hydrochloride exhibits cytotoxicity at concentrations of 0.05-1.0 mg/ml against mouse lung cancer cells (3LL) and human prostate cancer cells (DU-145), as well as other cancer cell lines including breast, gastric, ovarian, and non-Hodgkin's lymphoma[1].
Idazoxan hydrochloride has shown efficacy in reversing fluphenazine-induced catalepsy in male CD-COBS rats when subcutaneously injected at doses ranging from 0.16 to 5 mg/kg for a duration of 1 hour, with an ED50 of 0.25 mg/kg[3]. Intrathecal injection of Idazoxan hydrochloride (30 µg/10 µL) in SNL6W rats can enhance the endogenous analgesic index NSIA following 7,8-DHF treatment[4].
[1]. GF Eilon, L Weisenthal, M Stupecky,et al. Antineoplastic activity of idazoxan hydrochloride.[J]. Cancer Chemotherapy and Pharmacology,2009(64),1157-1163.
[2]. Bousquet P, et al. Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs. Ann N Y Acad Sci. 1999 Jun 21;881:272-8.
[3]. Roberto W Invernizzi, et al. The α2-Adrenoceptor Antagonist Idazoxan Reverses Catalepsy Induced by Haloperidol in Rats Independent of Striatal Dopamine Release: Role of Serotonergic Mechanisms. Neuropsychopharmacology volume 28, 2003: 872-879.
[4]. Kato D , Suto T , Obata H ,et al. Spinal Activation of Tropomyosin Receptor Kinase-B Recovers the Impaired Endogenous Analgesia in Neuropathic Pain Rats.[J].Anesth Analg, 2019(2).
[5]. Manji H K , Chen G , Bitran J A ,et al. Idazoxan down-regulates beta-adrenoceptors on C6 glioma cells in vitro.[J].European Journal of Pharmacology Molecular Pharmacology, 1992, 227(3):275-282.
盐酸咪唑克生（Idazoxan hydrochloride ，RX 781094 hydrochloride ，IDA）是一种分子量为241的α2-肾上腺和咪唑啉受体配体[1]。它与线粒体膜结合并促进胰腺β细胞的凋亡, 还可竞争性地拮抗唑啉样活性分子 (IMs) 的中枢性降压作用[2]。盐酸咪唑克生还可改善帕金森病、左旋多巴诱导的运动障碍和实验性帕金森综合征的运动症状。
在体外，用10 μM盐酸咪唑克生孵育大鼠神经胶质瘤C6细胞5天，可使β-肾上腺素受体数目减少23%，异丙肾上腺素诱导的cAMP蓄积减少37%[5]。此外，盐酸咪唑克生在0.05-1.0 mg/ml的浓度下对鼠肺癌细胞3LL和人前列腺癌细胞DU-1453都具有细胞毒性，且对乳腺癌、胃癌、肺癌、卵巢癌和前列腺癌以及非霍奇金淋巴瘤的等分试样也具有细胞毒性[1] 。
在体内，雄性CD-COBS大鼠皮下注射盐酸咪唑克生0.16-5 mg/kg，持续1小时治疗，可以有效逆转氟哌啶醇诱导的僵住症，ED50为0.25 mg/kg[3]。SNL6W大鼠鞘内注射盐酸咪唑克生（30 µ g/10 µL）可以提高7,8-DHF 治疗的内源性镇痛指标NSIA[4]。
| Cas No. | 79944-56-2 | SDF | |
| 别名 | 盐酸咪唑克生 | ||
| 化学名 | (S)-2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride | ||
| Canonical SMILES | [C@@H]1(C2=NCCN2)OC3=CC=CC=C3OC1.Cl | ||
| 分子式 | C11H12N2O2.HCl | 分子量 | 240.69 |
| 溶解度 | <24.07mg/ml in Water | 储存条件 | Store at 2-8°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1547 mL | 20.7736 mL | 41.5472 mL |
| 5 mM | 0.8309 mL | 4.1547 mL | 8.3094 mL |
| 10 mM | 0.4155 mL | 2.0774 mL | 4.1547 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。
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