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Tetracyclic antidepressants (TeCAs) are a class of antidepressants that were first introduced in the 1970s. They are named after their chemical structure, which contains four rings of atoms, and are closely related to the tricyclic antidepressants (TCAs), which contain three rings of atoms.

List of TeCAs

The TeCAs include the following agents:

• Marketed
  • Maprotiline (Deprilept, Ludiomil, Psymion)
  • Mianserin (Bolvidon, Norval, Tolvon)
  • Mirtazapine (Remeron, Avanza, Zispin)
  • Pirlindole (Pirazidol) — a tetracyclic reversible inhibitor of monoamine oxidase A (RIMA) used in Russia
  • Setiptiline (Tecipul)
• Not marketed
  • Aptazapine (CGS-7525A)
  • Metralindole — a tetracyclic RIMA investigated as an antidepressant
  • Esmirtazapine (ORG-50,081)
  • Oxaprotiline (C 49-802 BDA)
• Doubtful classification
  • Amoxapine (Asendin) — contains four, but not fused together rings; widely classified as a secondary amine tricyclic antidepressant
  • Ciclazindol (WY-23,409)
  • Loxapine (Loxapac, Loxitane, Adasuve) — a tricyclic antipsychotic with antidepressant properties; produces amoxapine as an active metabolite
  • Mazindol (Mazanor, Sanorex)

Pharmacology

Binding profiles

The affinities (K_d (nM)) of a selection of TeCAs have been compared below at an assortment of binding sites:

The selected ligands act as antagonists (or inverse agonists depending on the site in question) at all receptors listed and as inhibitors of all transporters listed.

References

1. Brunton, Laurence (2011). Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th Edition. China: McGraw-Hill. pp. 406–410. ISBN 978-0-07-162442-8.
2. Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology. 340 (2–3): 249–258. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821.{{cite journal}}: CS1 maint: multiple names: authors list (link)
3. Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology. 132 (2–3): 115–121. doi:10.1016/0014-2999(86)90596-0. PMID 3816971.{{cite journal}}: CS1 maint: multiple names: authors list (link)
4. Richelson E, Nelson A (July 1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". The Journal of Pharmacology and Experimental Therapeutics. 230 (1): 94–102. PMID 6086881.
5. Tatsumi M, Jansen K, Blakely RD, Richelson E (March 1999). "Pharmacological profile of neuroleptics at human monoamine transporters". European Journal of Pharmacology. 368 (2–3): 277–283. doi:10.1016/S0014-2999(99)00005-9. PMID 10193665.{{cite journal}}: CS1 maint: multiple names: authors list (link)
6. Wander TJ, Nelson A, Okazaki H, Richelson E (November 1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro". European Journal of Pharmacology. 143 (2): 279–282. doi:10.1016/0014-2999(87)90544-9. PMID 2891550.{{cite journal}}: CS1 maint: multiple names: authors list (link)
7. Richelson E, Nelson A (August 1984). "Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro". European Journal of Pharmacology. 103 (3–4): 197–204. doi:10.1016/0014-2999(84)90478-3. PMID 6149136.
8. Fernández J, Alonso JM, Andrés JI, et al. (March 2005). "Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents". Journal of Medicinal Chemistry. 48 (6): 1709–12. doi:10.1021/jm049632c. PMID 15771415.
9. de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM (April 1988). "Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers". Neuropharmacology. 27 (4): 399–408. doi:10.1016/0028-3908(88)90149-9. PMID 3419539.{{cite journal}}: CS1 maint: multiple names: authors list (link)

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