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Idazoxan hydrochloride Sale

(Synonyms: 盐酸咪唑克生) 目录号 : GC15813

Idazoxan hydrochlorideRX 781094 hydrochloride)是一种α2-肾上腺素受体拮抗剂,也是咪唑啉受体(IRs)的拮抗剂。

Idazoxan hydrochloride Chemical Structure

Cas No.:79944-56-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥495.00
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5mg
¥450.00
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10mg
¥720.00
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25mg
¥1,350.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

C6 glioma cells

Preparation method

Incubation of the C6 cells with 10 μM idazoxan for 5 days

Reaction Conditions

10 μM;5 days

Applications

in vitro resulted in a 23% reduction of β-adrenoceptor number and a 37% decrease in isoproterenol-induced cyclic AMP accumulation.

Animal experiment [2]:

Animal models

SNL6W rats

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. 

Dosage form

30 µg/10 µ L

Applications

Idazoxan blocked the 7,8-DHF–induced enhancement of NSIA in SNL6W rats (P < .001).

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).

产品描述

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241α2-肾上腺咪唑啉受体配体[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,ED500.25 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]

Chemical Properties

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
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溶解性数据

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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
240.69
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