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Tetracyclic antidepressants (TeCAs) are a class of drugs used primarily as 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:

• Pharmaceutical Drugs
  • Amoxapine (Asendin)
  • Maprotiline (Deprilept, Ludiomil, Psymion)
  • Mazindol (Mazanor, Sanorex)
  • Mianserin (Bolvidon, Norval, Tolvon)
  • Mirtazapine (Remeron, Avanza, Zispin)
  • Setiptiline (Tecipul)
• Research Chemicals
  • Aptazapine (CGS-7525A)
  • Ciclazindol (WY-23,409)
  • Esmirtazapine (ORG-50,081)
  • Oxaprotiline

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.

See also

• Tricyclic antidepressant (TCA)

References

1. Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology. 340 (2–3): 249–58. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
2. Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology. 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
3. Richelson E, Nelson A (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. {{cite journal}}: Unknown parameter |month= ignored (help)
4. Tatsumi M, Jansen K, Blakely RD, Richelson E (1999). "Pharmacological profile of neuroleptics at human monoamine transporters". European Journal of Pharmacology. 368 (2–3): 277–83. doi:10.1016/S0014-2999(99)00005-9. PMID 10193665. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
5. Wander TJ, Nelson A, Okazaki H, Richelson E (1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro". European Journal of Pharmacology. 143 (2): 279–82. doi:10.1016/0014-2999(87)90544-9. PMID 2891550. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
6. Richelson E, Nelson A (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. {{cite journal}}: Unknown parameter |month= ignored (help)
7. Fernández J, Alonso JM, Andrés JI; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
8. de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM (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}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)

• Tetracyclic antidepressants