四环类抗抑郁药
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四环抗抑郁药（英语：tetracyclic antidepressants，缩写作 TeCAs）是一种在1970s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。
四环抗忧郁药清单
[编辑]如下:
- 已上市
- Maprotiline (Deprilept, Ludiomil, Psymion)
- 米塞林 (Bolvidon, Norval, Tolvon)
- 米氮平 (Remeron, Avanza, Zispin)
- Pirlindole (Pirazidol) — 在俄罗斯使用的四环可逆单胺氧化酶A抑制剂 (RIMA)
- Setiptiline (Tecipul)
- 未上市
- Aptazapine (CGS-7525A)
- Metralindole — 一个四环的可逆单胺氧化酶A抑制剂
- Esmirtazapine (ORG-50,081)
- Oxaprotiline (C 49-802 BDA)
药理学
[编辑]结合特性
[编辑]以下比较四环抗忧郁药对各结合位点的亲和性 (Kd (nM)):[1][2][3][4][5][6][7][8][9]
| 化合物 | SERT | NET | DAT | 5-HT1A | 5-HT2A | α1 | α2 | D2 | H1 | mACh |
| Amoxapine | 58 | 16.0 | 4,310 | 220 | 0.6 | 50 | 2,600 | 160 | 25 | 1,000 |
| Loxapine | 2,400 | 380 | 9,000 | 2,900 | 1.7 | 28 | 2,400 | 70 | 4.9 | 450 |
| 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 | 3,900 | 4.9 | 4,340 | 67,000 | 2,400 | 620 | 42,000 | ? | 21 | 2,900 |
以上化合物于受体可能作为受体拮抗剂 (或反激动剂，视结合位点而定)，于膜上转运蛋白作为再摄取抑制剂。
参考文献
[编辑]- ^ Brunton, Laurence. Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th Edition. China: McGraw-Hill. 2011: 406–410. ISBN 978-0-07-162442-8.
- ^ 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 [2016-03-25]. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. （原始内容存档于2021-02-24）.
- ^ 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.
- ^ 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 [2016-03-25]. PMID 6086881. （原始内容存档于2021-08-28）.
- ^ 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.
- ^ 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 [2016-03-25]. PMID 2891550. doi:10.1016/0014-2999(87)90544-9. （原始内容存档于2019-05-17）.
- ^ 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.
- ^ Fernández J, Alonso JM, Andrés JI, et al. 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.
- ^ 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.