四环类抗抑郁药

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四环类抗抑郁药米氮平的化学结构, 其结构有四个原子环

四环抗抑郁药英语:Tetracyclic antidepressants,缩写TeCAs)是一种在1907s被引入的抗抑郁药。他们是因其化学结构含有四个原子环而命名,与三环抗抑郁药紧密相关,即含有三个原子环

四環抗憂鬱藥清單[编辑]

如下:

藥理學[编辑]

結合特性[编辑]

以下比較四環抗憂鬱藥對各結合位點英语binding site親和性 (Kd (nM)):[1][2][3][4][5][6][7][8][9]

化合物 SERT NET DAT 5-HT1A英语5-HT1A receptor 5-HT2A英语5-HT2A receptor α1英语alpha-1 adrenergic receptor α2英语alpha-2 adrenergic receptor D2 H1英语H1 receptor mACh
Amoxapine英语Amoxapine 58 16.0 4,310 220 0.6 50 2,600 160 25 1,000
Loxapine英语Loxapine 2,400 380 9,000 2,900 1.7 28 2,400 70 4.9 450
Maprotiline英语Maprotiline 5,800 11.1 1,000 12,000 120 91 9,400 350 2.0 560
米塞林 4,000 101 9,400 190 4.3 74 4.3 2,197 1.7 820
米氮平 >100,000 1,640 >100,000  ? 69 500 19 >5,454 0.1 670
Oxaprotiline英语Oxaprotiline 3,900 4.9 4,340 67,000 2,400 620 42,000  ? 21 2,900

以上化合物於受體可能作為受体拮抗剂 (或反激动剂,視結合位點而定),於膜上轉運蛋白作為再攝取抑制劑


參見[编辑]


參考資料[编辑]

  1. ^ Brunton, Laurence. Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th Edition. China: McGraw-Hill. 2011: 406–410. ISBN 978-0-07-162442-8. 
  2. ^ Tatsumi M, Groshan K, Blakely RD, Richelson E. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. European Journal of Pharmacology. December 1997, 340 (2–3): 249–258. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. 
  3. ^ Wander TJ, Nelson A, Okazaki H, Richelson E. Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro. European Journal of Pharmacology. December 1986, 132 (2–3): 115–121. PMID 3816971. doi:10.1016/0014-2999(86)90596-0. 
  4. ^ Richelson E, Nelson A. Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro. The Journal of Pharmacology and Experimental Therapeutics. July 1984, 230 (1): 94–102. PMID 6086881. 
  5. ^ Tatsumi M, Jansen K, Blakely RD, Richelson E. Pharmacological profile of neuroleptics at human monoamine transporters. European Journal of Pharmacology. March 1999, 368 (2–3): 277–283. PMID 10193665. doi:10.1016/S0014-2999(99)00005-9. 
  6. ^ Wander TJ, Nelson A, Okazaki H, Richelson E. Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro. European Journal of Pharmacology. November 1987, 143 (2): 279–282. PMID 2891550. doi:10.1016/0014-2999(87)90544-9. 
  7. ^ Richelson E, Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. European Journal of Pharmacology. August 1984, 103 (3–4): 197–204. PMID 6149136. doi:10.1016/0014-2999(84)90478-3. 
  8. ^ Fernández J, Alonso JM, Andrés JI, 等. Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. Journal of Medicinal Chemistry. March 2005, 48 (6): 1709–12. PMID 15771415. doi:10.1021/jm049632c. 
  9. ^ de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM. Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers. Neuropharmacology. April 1988, 27 (4): 399–408. PMID 3419539. doi:10.1016/0028-3908(88)90149-9. 

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