N-乙酰血清素
N-乙酰血清素（英文名：N-Acetylserotonin，NAS，也作normelatonin）是一种天然存在的化合物，是从血清素到褪黑素的内源性合成的反应中间体[1][2]。它由血清素（又称为5-羟色胺）在N-乙酰基转移酶（AANAT）催化下与乙酰辅酶A反应产生，然后N-乙酰血清素再在乙酰血清素O-甲基转移酶（ASMT）催化下被S-腺苷甲硫氨酸甲基化为褪黑素。和褪黑素一样，N-乙酰血清素也是褪黑素受体（褪黑素受体1A、褪黑素受体1B和褪黑素受体1C）的激动剂，并且可以被认为是一种神经递质。[3][4][5][6]
最近，NAS已经显示出作为一种有效力的TrkB受体激动剂，而血清素和褪黑激素并没有此种机制。[3] 以"TrkB受体"为介导(TrkB-mediated)而产生出强劲的抗抑郁，神经保护(neuroprotection)和神经营养因子等效果。[3]
此外，光线照射抑制NAS的合成、和减少单胺氧化抑制剂的抗抑郁作用。[3] 这些数据强烈支持NAS在调节情绪和引起抗抑郁药的治疗效益之作用。
通过目前未知的机制，NAS可能是姿位性低血压的引发因子、且以"单胺氧化抑制剂"(MAOIs)作临床治疗。[7][8] It reduces blood pressure in rodents, and pinealectomy (the pineal gland being a major site of NAS and melatonin synthesis) abolishes the hypotensive effects of clorgyline.[7][8] 为什么"姿位性低血压"常见与"单胺氧化抑制剂"(MAOIs)一起发生，而不与SSRIs(这两者均增加NAS级别)一起，而这方面并不清楚。
另见
参考文献
- ↑ AXELROD J, WEISSBACH H. Enzymatic O-methylation of N-acetylserotonin to melatonin. Science. April 1960, 131 (3409): 1312. Error: Bad DOI specified模板:Namespace detect showall. PMID 13795316.
- ↑ WEISSBACH H, REDFIELD BG, AXELROD J. Biosynthesis of melatonin: enzymic conversion of serotonin to N-acetylserotonin. Biochimica et Biophysica Acta. September 1960, 43: 352–3. Error: Bad DOI specified模板:Namespace detect showall. PMID 13784117.
- ↑ 3.0 3.1 3.2 3.3 Jang SW, Liu X, Pradoldej S, et al.. N-acetylserotonin activates TrkB receptor in a circadian rhythm. Proceedings of the National Academy of Sciences of the United States of America. February 2010, 107 (8): 3876. Error: Bad DOI specified模板:Namespace detect showall. PMID 20133677. PMC 2840510.
- ↑ Zhao H, Poon AM, Pang SF. Pharmacological characterization, molecular subtyping, and autoradiographic localization of putative melatonin receptors in uterine endometrium of estrous rats. Life Sciences. March 2000, 66 (17): 1581–91. Error: Bad DOI specified模板:Namespace detect showall. PMID 11261588.
- ↑ Nonno R, Pannacci M, Lucini V, Angeloni D, Fraschini F, Stankov BM. [http//www.ncbi.nlm.nih.gov/pmc/articles/PMC1566130/ Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1-antagonists]. British Journal of Pharmacology. July 1999, 127 (5): 1288–94. Error: Bad DOI specified模板:Namespace detect showall. PMID 10455277. PMC 1566130.
- ↑ Paul P, Lahaye C, Delagrange P, Nicolas JP, Canet E, Boutin JA. Characterization of 2-[125Iiodomelatonin binding sites in Syrian hamster peripheral organs]. The Journal of Pharmacology and Experimental Therapeutics. July 1999, 290 (1): 334–40. PMID 10381796.
- ↑ 7.0 7.1 Oxenkrug GF. [N-acetylserotonin and hypotensive effect of MAO-A inhibitors]. Voprosy Meditsinskoi Khimii. 1997, 43 (6): 522–6. PMID 9503569 (Russian).
- ↑ 8.0 8.1 引用错误：无效
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模板:神经递质
模板:Melatonergics
模板:色胺