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'''Tetracyclic antidepressants''' ('''TeCAs''') are a [[chemical class|class]] of [[psychoactive drug|drug]]s used primarily as [[antidepressant]]s that were first introduced in the 1970s. They are named after their [[chemical structure]] which contains four [[cyclic compound|rings of atom]]s and are closely related to the [[tricyclic antidepressant]]s (TCAs) which contain three rings of atoms.
'''Tetracyclic antidepressants''' ('''TeCAs''') are a [[chemical class|class]] of [[psychoactive drug|drug]]s used primarily as [[antidepressant]]s that were first introduced in the 1970s. They are named after their [[chemical structure]] which contains four [[cyclic compound|rings of atom]]s and are closely related to the [[tricyclic antidepressant]]s (TCAs) which contain three rings of atoms.


== List of TeCAs ==
a number in the German language== List of TeCAs ==


The TeCAs include the following agents:
The TeCAs include the following agents:

Revision as of 01:08, 20 May 2010

Not to be confused with Tetracycline.
Chemical structure of the tetracyclic antidepressant amoxapine. Notice its four rings.

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.

a number in the German language== List of TeCAs ==

The TeCAs include the following agents:

Pharmacology

Binding profiles

The affinities (Kd (nM)) of a selection of TeCAs have been compared below at an assortment of binding sites:[1][2][3][4][5][6][7][8]

Compound SERT NET DAT 5-HT1A 5-HT2A 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 90 9,400 350 2.0 570
Mianserin 4,000 101 9,400 190 4.3 74 4.3 2,197 1.7 820
Mirtazapine >100,000 1,640 >100,000 ? 69 608 19 >5,454 1.6 794
Oxaprotiline 3,900 4.9 4,340 67,000 2,400 620 42,000 ? 21 2,900

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

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. 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. 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. 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. 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. 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. PMID 3419539. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)



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