四环类抗抑郁药

四环抗抑郁药（英語：，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。

四环类抗抑郁药米氮平的化学结构, 其结构有四个原子环

四環抗憂鬱藥清單

如下:

已上市
- Maprotiline (Deprilept, Ludiomil, Psymion)
- 米塞林 (Bolvidon, Norval, Tolvon)
- 米氮平 (Remeron, Avanza, Zispin)
- Pirlindole (Pirazidol) — 在俄羅斯使用的四環可逆單胺氧化酶A抑制劑 (RIMA)
- Setiptiline (Tecipul)
未上市
- Aptazapine (CGS-7525A)
- Metralindole — 一個四環的可逆單胺氧化酶A抑制劑
- Esmirtazapine (ORG-50,081)
- Oxaprotiline (C 49-802 BDA)

藥理學

結合特性

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

化合物	SERT	NET	DAT	5-HT_1A	5-HT_2A	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。

参考文献

Brunton, Laurence. . China: McGraw-Hill. 2011: 406–410. ISBN 978-0-07-162442-8.
Tatsumi M, Groshan K, Blakely RD, Richelson E. . 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. . 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. . 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. . 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. . 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. . 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. . 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. . Neuropharmacology. April 1988, 27 (4): 399–408. PMID 3419539. doi:10.1016/0028-3908(88)90149-9.

#invoke:navbox Template:Hypnotics and sedatives

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[Goodman-1] Brunton, Laurence. . China: McGraw-Hill. 2011: 406–410. ISBN 978-0-07-162442-8.

[pmid9537821-2] Tatsumi M, Groshan K, Blakely RD, Richelson E. . 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）.

[pmid3816971-3] Wander TJ, Nelson A, Okazaki H, Richelson E. . European Journal of Pharmacology. December 1986, 132 (2–3): 115–121. PMID 3816971. doi:10.1016/0014-2999(86)90596-0.

[pmid6086881-4] Richelson E, Nelson A. . 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）.

[pmid10193665-5] Tatsumi M, Jansen K, Blakely RD, Richelson E. . European Journal of Pharmacology. March 1999, 368 (2–3): 277–283. PMID 10193665. doi:10.1016/S0014-2999(99)00005-9.

[pmid2891550-6] Wander TJ, Nelson A, Okazaki H, Richelson E. . 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）.

[pmid6149136-7] Richelson E, Nelson A. . European Journal of Pharmacology. August 1984, 103 (3–4): 197–204. PMID 6149136. doi:10.1016/0014-2999(84)90478-3.

[pmid15771415-8] Fernández J, Alonso JM, Andrés JI, et al. . Journal of Medicinal Chemistry. March 2005, 48 (6): 1709–12. PMID 15771415. doi:10.1021/jm049632c.

[pmid3419539-9] Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM. . Neuropharmacology. April 1988, 27 (4): 399–408. PMID 3419539. doi:10.1016/0028-3908(88)90149-9.