盐酸咪唑克生

中文名称:

盐酸咪唑克生

中文同义词:

盐酸咪唑克生;咪唑克生盐酸盐

英文名称:

IDAZOXAN HYDROCHLORIDE

英文同义词:

(+/-)-Idazoxan Monohydrochloride;2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-iMidazole Hydrochloride;RX 781094A;2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-iMidazole hydrochloride;IDAZOXAN HYDROCHLORIDE;2-(1,4-BENZODIOXAN-2-YL)-2-IMIDAZOLINE HYDROCHLORIDE;IdazoxanHCl;RX 781094, (±)-2-[1,4-Benzodioxan-2-yl]-2-imidazoline hydrochloride

CAS号:

79944-56-2

分子式:

C11H13ClN2O2

分子量:

240.69

EINECS号:

相关类别:

小分子抑制剂;有机中间体;Adrenoceptor;Aromatics;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals

Mol文件:

79944-56-2.mol

熔点

207-208°

储存条件

Store at RT

溶解度

H2O: 300 mg/mL

生物活性

Idazoxan hydrochloride (RX 781094 hydrochloride) 是一种 α2-肾上腺素受体拮抗剂，也是咪唑啉受体 (IRs) 拮抗剂，可竞争性拮抗唑啉样药物 (IMs) 的中枢性降压作用。Idazoxan hydrochloride 还可改善帕金森氏病，L-DOPA 引起的运动障碍和实验性帕金森病的运动症状。

靶点

α 2 -adrenoceptor; Imidazoline receptors (IRs)

体内研究

Idazoxan (0.16-5 mg/kg; subcutaneous injection; for 1 hour; male CD-COBS rats) treatment potently reverses haloperidol-induced catalepsy with an ED 50 of 0.25 mg/kg. Idazoxan (0.3 and 2.5 mg/kg) has no effect on extracellular DA and do not modify the rise of extracellular DA induced by haloperidol. Animal Model: Male CD-COBS rats injected with 1 mg/kg haloperidol Dosage: 0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0 mg/kg Administration: Subcutaneous injection; for 1 hour Result: Potently reversed haloperidol-induced catalepsy with an ED 50 of 0.25 mg/kg.

Animal Model:

Male CD-COBS rats injected with 1 mg/kg haloperidol

Dosage:

0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0 mg/kg

Administration:

Subcutaneous injection; for 1 hour

Result:

Potently reversed haloperidol-induced catalepsy with an ED 50 of 0.25 mg/kg.

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