(±)-Acetylcarnitine chloride

(±)-Acetylcarnitine chloride是一种胆碱能激动剂.

乙酰胆碱受体(AChR)是一种乙酰胆碱的整合膜蛋白受体.AChRs有两种:烟碱乙酰胆碱受体和毒蕈碱乙酰胆碱受体.

(±)-Acetylcarnitine chloride是一种胆碱能激动剂和脂质代谢的中间产物[1].在视网膜神经节细胞中,乙酰肉碱和乙酰胆碱抑制GABA能应答外源性GABA和GABA能抑制性突触后电流[2].

在冠状动脉结扎的犬中,(-)-肉碱氯化物(LCC)(300 mg/kg)和乙酰基(-)-肉碱氯化物(ALCC)(300 mg/kg)抑制室性心律失常.另外,LCC和ALCC改善氧化磷酸化率和线粒体功能[1].在小鼠热板试验中,乙酰左旋肉碱(ALCAR)(100 mg/kg)表现出镇痛作用.同时,U-73122和新霉素(磷脂酶C(PLC)抑制剂)阻断ALCAR诱导的痛阈的增加.损害磷脂合成的LiCl剂量依赖性地拮抗镇痛作用.PMA和PDBu(PKC活化剂)剂量依赖性地阻断痛阈增加.这些结果表明,ALCAR镇痛需要PLC-IP3途径的参与[3].

参考文献：
[1].  Imai S, Matsui K, Nakazawa M, et al. Anti-arrhythmic effects of (-)-carnitine chloride and its acetyl analogue on canine late ventricular arrhythmia induced by ligation of the coronary artery as related to improvement of mitochondrial function. Br J Pharmacol, 1984, 82(2): 533-542.
[2].  Bhring R, Standhardt H, Martelli EA, et al. GABA-activated chloride currents of postnatal mouse retinal ganglion cells are blocked by acetylcholine and acetylcarnitine: how specific are ion channels in immature neurons Eur J Neurosci, 1994, 6(7): 1089-1099.
[3].  Galeotti N, Bartolini A, Calvani M, et al. Acetyl-L-carnitine requires phospholipase C-IP3 pathway activation to induce antinociception. Neuropharmacology, 2004, 47(2): 286-294.