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四环抗抑郁药（英语：tetracyclic antidepressants，缩写作 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。
四环抗忧郁药清单
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
结合特性
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-HT1A]] | [[:5-HT2A|5-HT2A]] | [[:α1|α1]] | [[:α2|α2]] | D2 | [[:H1|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
- ↑ 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. 1997-12, 340 (2–3): 249–258. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9.
- ↑ 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. 1986-12, 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. 1984-07, 230 (1): 94–102. PMID 6086881.
- ↑ Tatsumi M, Jansen K, Blakely RD, Richelson E. Pharmacological profile of neuroleptics at human monoamine transporters. European Journal of Pharmacology. 1999-03, 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. 1987-11, 143 (2): 279–282. PMID 2891550. doi:10.1016/0014-2999(87)90544-9.[失效链接]
- ↑ Richelson E, Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. European Journal of Pharmacology. 1984-08, 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. 2005-03, 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. 1988-04, 27 (4): 399–408. PMID 3419539. doi:10.1016/0028-3908(88)90149-9.