一般的麻醉药物异丙酚增加大脑N-arachidonylethanolamine (anandamide)内容和抑制脂肪酸酰胺水解酶。
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Patel, Wohlfeil呃,随处DJ,航母EJ,佩里LJ,茶室,Falck JR Nithipatikom K,坎贝尔WB,希拉德CJ
一般的麻醉药物异丙酚增加大脑N-arachidonylethanolamine (anandamide)内容和抑制脂肪酸酰胺水解酶。
Br J杂志。2003年7月,139(5):1005 - 13所示。
- PubMed ID
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12839875 (在PubMed]
- 文摘
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1。6-diisopropylphenol异丙酚(2)是广泛使用的全身麻醉剂和维护长期镇静。我们已经测试了异丙酚的假设改变大脑神经的内容,这种效应导致其镇静特性。2。镇静剂量的异丙酚对小鼠产生了显著增加整个大脑神经的的内容,N-arachidonylethanolamine (anandamide),当腹腔内接种Intralipid或emulphor-ethanol车辆。3所示。在体外,异丙酚是一个竞争性抑制剂(IC(50) 52微米;95%置信区间31,87)的脂肪酸酰胺水解酶(FAAH),催化降解的anandamide。在一系列的异丙酚类似物,FAAH抑制的关键结构的决定因素和镇静作用被发现重叠。其他静脉全身麻醉药,包括咪达唑仑,氯胺酮,依托咪酯,硫喷妥钠,不影响FAAH活动sedative-relevant浓度。 Thiopental, however, is a noncompetitive inhibitor of FAAH at a concentration of 2 mM. 4. Pretreatment of mice with the CB(1) receptor antagonist SR141716 (1 mg kg(-1), i.p.) significantly reduced the number of mice that lost their righting reflex in response to propofol. Pretreatment of mice with the CB(1) receptor agonist, Win 55212-2 (1 mg kg(-1), i.p.), significantly potentiated the loss of righting reflex produced by propofol. These data indicate that CB(1) receptor activity contributes to the sedative properties of propofol. 5. These data suggest that propofol activation of the endocannabinoid system, possibly via inhibition of anandamide catabolism, contributes to the sedative properties of propofol and that FAAH could be a novel target for anesthetic development.