N-乙酰血清素（英語：N-Acetylserotonin，NAS，也作normelatonin）是一種天然存在的化合物，是從血清素到褪黑素的內源性合成的反應中間體[1][2]。它由血清素（又稱為5-羥色胺）在N-乙?；D移酶（AANAT）催化下與乙酰輔酶A反應產生，然后N-乙酰血清素再在乙酰血清素O-甲基轉移酶（ASMT）催化下被S-腺苷甲硫氨酸甲基化為褪黑素。和褪黑素一樣，N-乙酰血清素也是褪黑素受體（褪黑素受體1A、褪黑素受體1B和褪黑素受體1C）的激動劑，并且可以被認為是一種神經遞質。[3][4][5][6]
最近，NAS已經顯示出作為一種有效力的TrkB受體激動劑，而血清素和褪黑激素并沒有此種機制。[3] 以"TrkB受體"為介導(TrkB-mediated)而產生出強勁的抗抑郁，神經保護(neuroprotection)和神經營養(yǎng)因子等效果。[3]
此外，光線照射抑制NAS的合成、和減少單胺氧化抑制劑的抗抑郁作用。[3] 這些數(shù)據(jù)強烈支持NAS在調節(jié)情緒和引起抗抑郁藥的治療效益之作用。
通過目前未知的機制，NAS可能是姿位性低血壓的引發(fā)因子、且以"單胺氧化抑制劑"(MAOIs)作臨床治療。[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] 為什么"姿位性低血壓"常見與"單胺氧化抑制劑"(MAOIs)一起發(fā)生，而不與SSRIs(這兩者均增加NAS級別)一起，而這方面并不清楚。
另見
參考文獻
- ↑ AXELROD J, WEISSBACH H. Enzymatic O-methylation of N-acetylserotonin to melatonin. Science. April 1960, 131 (3409): 1312. doi:10.1126/science.131.3409.1312. 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. doi:10.1016/0006-3002(60)90453-4. 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. doi:10.1073/pnas.0912531107. 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. doi:10.1016/S0024-3205(00)00478-1. 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. doi:10.1038/sj.bjp.0702658. 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).
- ↑ 引用錯誤：無效
<ref>標簽；未為name屬性為pmid10591054的引用提供文字
|
|
|
| 直接衍生物 |
|
|
氨基N-取代
衍生物 |
|
|
氨基N,N-二取代
衍生物 |
|
|
參考來源
更多醫(yī)學百科條目
訂閱討論RSS