- 生物活性
盐酸咪唑克生(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。其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.
