四環類抗抑鬱藥

四環抗抑鬱藥（英語：tetracyclic antidepressants，縮寫作 TeCAs）是一種在1970s被引入的抗抑鬱藥。他們是因其化學結構含有四個原子環而命名，與三環抗抑鬱藥緊密相關，即含有三個原子環。

四環抗憂鬱藥清單

如下:

已上市
- Maprotiline（英語：Maprotiline） (Deprilept, Ludiomil, Psymion)
- 米塞林 (Bolvidon, Norval, Tolvon)
- 米氮平 (Remeron, Avanza, Zispin)
- Pirlindole（英語：Pirlindole） (Pirazidol) — 在俄羅斯使用的四環可逆單胺氧化酶A抑制劑 (RIMA)
- Setiptiline（英語：Setiptiline） (Tecipul)
未上市
- Aptazapine（英語：Aptazapine） (CGS-7525A)
- Metralindole（英語：Metralindole） — 一個四環的可逆單胺氧化酶A抑制劑
- Esmirtazapine（英語：Esmirtazapine） (ORG-50,081)
- Oxaprotiline（英語：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（英語：5-HT1A receptor）	5-HT_2A（英語：5-HT2A receptor）	α₁（英語：alpha-1 adrenergic receptor）	α₂（英語：alpha-2 adrenergic receptor）	D₂	H₁（英語：H1 receptor）	mACh
Amoxapine（英語：Amoxapine）	58	16.0	4,310	220	0.6	50	2,600	160	25	1,000
Loxapine（英語：Loxapine）	2,400	380	9,000	2,900	1.7	28	2,400	70	4.9	450
Maprotiline（英語：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（英語：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體拮抗劑 (或反激動劑，視結合位點而定)，於膜上轉運蛋白作為再攝取抑制劑。

參考文獻

^ 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. （原始內容存檔於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. （原始內容存檔於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. （原始內容存檔於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.

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[Goodman-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.

[pmid9537821-2] 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 [2016-03-25]. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. （原始內容存檔於2021-02-24）.

[pmid3816971-3] 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.

[pmid6086881-4] 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 [2016-03-25]. PMID 6086881. （原始內容存檔於2021-08-28）.

[pmid10193665-5] 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.

[pmid2891550-6] 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 [2016-03-25]. PMID 2891550. doi:10.1016/0014-2999(87)90544-9. （原始內容存檔於2019-05-17）.

[pmid6149136-7] 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.

[pmid15771415-8] 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.

[pmid3419539-9] 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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