79944-56-2
中文名称
盐酸咪唑克生
英文名称
IDAZOXAN HYDROCHLORIDE
CAS
79944-56-2
分子式
C11H13ClN2O2
分子量
240.69
MOL 文件
79944-56-2.mol
更新日期
2024/08/10 09:04:06
79944-56-2 结构式
基本信息
中文别名
盐酸咪唑克生咪唑克生盐酸盐
英文别名
RX 781094AIdazoxanHCl
IDAZOXAN HYDROCHLORIDE
(+/-)-Idazoxan Monohydrochloride
2-(1,4-BENZODIOXAN-2-YL)-2-IMIDAZOLINE HYDROCHLORIDE
RX 781094, (±)-2-[1,4-Benzodioxan-2-yl]-2-imidazoline hydrochloride
Idazoxan hydrochloride,2-(1,4-Benzodioxan-2-yl)-2-imidazolinehydrochloride
2-(2,3-Dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-iMidazole Hydrochloride
2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-iMidazole hydrochloride
所属类别
生物化工：激动剂抑制剂物理化学性质
熔点207-208°
储存条件Store at RT
溶解度H2O: 300 mg/mL
形态Powder
颜色White to off-white
水溶解性Soluble to 100 mM in water
稳定性Hygroscopic
常见问题列表
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. |