Cannabimimetic Activity, Binding, and Degradation of Stearoylethanolamide within the Mouse Central Nervous System
Cannabimimetic Activity, Binding, and Degradation of Stearoylethanolamide within the Mouse Central Nervous System
复制标题
小鼠中枢神经系统内硬脂酰乙醇酰胺的大麻模拟活性、结合和降解
DOI：
10.1006/mcne.2002.1164
复制
发表时间：
2002
影响因子：
3.5
通讯作者：
A. Finazzi
中科院分区：
文献类型：
--
作者：
M. Maccarrone;A. Cartoni;D. Parolaro;A. Margonelli;P. Massi;M. Bari;N. Battista;A. Finazzi
硬脂酰乙醇胺(SEA)存在于人、大鼠和小鼠的大脑中，其含量与内源性大麻酸乙醇胺(花生四烯基乙醇胺，AEA)相当。然而，海洋的生物活性从未被调查过。我们报道，SEA对小鼠的惊厥、运动、镇痛和体温具有相同的作用，SEA的特异性结合部位存在于小鼠大脑中，以皮质最丰富。药理实验和基因敲除小鼠的使用表明，这些位点不同于大麻素受体，不与G蛋白偶联，调节不同的信号通路。小鼠大脑也有一个特定的SEA膜转运体和一个能够裂解SEA的脂肪酸酰胺水解酶，其区域分布与这种脂类的结合部位相同。此外，SEA可增强AEA引起的小鼠脑片cAMP含量的降低，提示SEA可能也是一种“伴随性”化合物。
Stearoylethanolamide (SEA) is present in human, rat, and mouse brain in amounts comparable to those of the endocannabinoid anandamide (arachidonoylethanolamide, AEA). Yet, the biological activity of SEA has never been investigated. We report that SEA has the same effects as AEA on catalepsy, motility, analgesia, and body temperature of mice and that specific binding sites for SEA are present in mouse brain and are most abundant in cortex. Pharmacological experiments and the use of knockout mice demonstrated that these sites are different from cannabinoid receptors, are not coupled to G proteins, and regulate different signaling pathways. Mouse brain has also a specific SEA membrane transporter and a fatty acid amide hydrolase able to cleave SEA, with the same regional distribution as the binding sites of this lipid. Moreover, SEA potentiates the decrease of cAMP induced by AEA in mouse cortical slices, suggesting that SEA might also be an "entourage" compound.
登录
查看更多内容
影响因子：
3.4
作者：
P. Reggio;Hassimi Traore
通讯作者：
P. Reggio;Hassimi Traore
影响因子：
15.9
作者：
Deutsch, DG;Goligorsky, MS;Moore, LC
通讯作者：
Moore, LC
anandamide（一种假定的内源性大麻素）在小鼠中的药理活性。
DOI：
--
发表时间：
1994
期刊：
The Journal of pharmacology and experimental therapeutics
影响因子：
--
作者：
Smith,PB;Compton,DR;Welch,SP;Razdan,RK;Mechoulam,R;Martin,BR
通讯作者：
Martin,BR
影响因子：
13.6
作者：
Mechoulam, R;Panikashvili, D;Shohami, E
通讯作者：
Shohami, E
影响因子：
3.6
作者：
Breivogel, CS;Griffin, G;Martin, BR
通讯作者：
Martin, BR