BU 224 hydrochloride

BU 224 hydrochloride是一种选择性的咪唑啉I2受体的配体,Ki值为2.1 nM [1].

咪唑啉受体是可乐定和其他咪唑啉的主要受体.咪唑啉I2受体是单胺氧化酶的变构结合位点,在神经保护和疼痛调节中起关键作用.

BU 224 hydrochloride是一种选择性的咪唑啉I2受体的配体.在大鼠强迫游泳实验(FST)中,BU224显著抑制不动性并增加轻度游泳.此外,BU224增加肾上腺皮质激素(ACTH)应答FST和额皮质中5-羟色胺(5-HT)水平,并减少5-HT在下丘脑和额皮质中的周转.这些结果表明,BU224具有抗抑郁样活性[2].在黑质纹状体道单侧损伤大鼠中,BU224(14 mg/kg)显著增加同向性旋转[3].在大鼠温水缩尾试验中,BU224抑制2-BFI和胍丁胺诱导的吗啡和反胺苯环醇镇痛作用的增强[4].

参考文献：
[1].  Hudson AL, Gough R, Tyacke R, et al. Novel selective compounds for the investigation of imidazoline receptors. Ann N Y Acad Sci, 1999, 881: 81-91.
[2].  Finn DP, Martí O, Harbuz MS, et al. Behavioral, neuroendocrine and neurochemical effects of the imidazoline I2 receptor selective ligand BU224 in naive rats and rats exposed to the stress of the forced swim test. Psychopharmacology (Berl), 2003, 167(2): 195-202.
[3].  Macinnes N, Duty S. Locomotor effects of imidazoline I2-site-specific ligands and monoamine oxidase inhibitors in rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway. Br J Pharmacol, 2004, 143(8): 952-959.
[4].  Thorn DA, Zhang Y, Peng BW, et al. Effects of imidazoline I receptor ligands on morphine- and tramadol-induced antinociception in rats. Eur J Pharmacol, 2011, 670(2-3): 435-440.