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N-DOCOSAHEXAENOYL, 3 HYDROXYTYRAMINE - A DOPAMINERGIC COMPOUND THAT PENETRATES THE BLOOD-BRAIN BARRIER AND SUPPRESSES APPETITE

机译:N-DOCOSAHEXAENOYL,3羟基酪氨酸-一种渗透血脑屏障并抑制食欲的多巴胺化合物

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Fatty acids with varying chain lengths (2-22 carbon atoms long) and degrees of unsaturation (0-6 double bonds) were used to synthesize dopaminergic compounds for a study of the carrier mediated transport of dopamine (DA) to the brain. The most active carrier was the all cis C22:6 fatty acid [docosahexaenoic acid,( DHA)]which increased DA uptake through the blood-brain barrier by greater than 7.5 fold. The DHA-DA compound, NMI 8739, depressed the general locomotor activity of mice in a dose dependent manner. It also suppressed the appetite of Balb c mice and Charles River rats by 50% and 95% respectively at a dose of 10 mg/kg. Daily administration of NMI-8739 for a three week period did not induce tolerance. These results demonstrate DHA's potential for the carrier mediated transport of small molecules to the brain. [References: 17]
机译:具有可变链长(2-22个碳原子长)和不饱和度(0-6个双键)的脂肪酸用于合成多巴胺能化合物,以研究载体介导的多巴胺(DA)向大脑的转运。活性最高的载体是全顺式C22:6脂肪酸[二十二碳六烯酸((DHA)],它通过血脑屏障的DA摄取增加了7.5倍以上。 DHA-DA化合物NMI 8739以剂量依赖性方式抑制了小鼠的总体运动活性。它还以10 mg / kg的剂量分别抑制Balb c小鼠和Charles River大鼠的食欲50%和95%。连续三周每日服用NMI-8739不会引起耐受性。这些结果证明了DHA在载体介导的小分子向大脑转运方面的潜力。 [参考:17]

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