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** ] (Bolvidon, Norval, Tolvon) ** ] (Bolvidon, Norval, Tolvon)
** ] (Remeron, Avanza, Zispin) ** ] (Remeron, Avanza, Zispin)
** ] (Pirazidol) — a tetracyclic ] (RIMA) used in Russia ** ] (Pirazidol) – a tetracyclic ] (RIMA) used in Russia
** ] (Tecipul) ** ] (Tecipul)
* Not marketed * Not marketed
** ] (CGS-7525A) ** ] (CGS-7525A)
** ] — a tetracyclic RIMA investigated as an antidepressant ** ] – a tetracyclic RIMA investigated as an antidepressant
** ] (ORG-50,081) ** ] (ORG-50,081)
**] (4 rings) **] (4 rings)
** ] (C 49-802 BDA) ** ] (C 49-802 BDA)
* Doubtful classification * Doubtful classification
** ] (Asendin) — contains four, but not fused together rings; widely classified as a secondary amine tricyclic antidepressant ** ] (Asendin) – contains four, but not fused together rings; widely classified as a secondary amine tricyclic antidepressant
** ] (WY-23,409) ** ] (WY-23,409)
** ] (Loxapac, Loxitane, Adasuve) — a tricyclic ] with antidepressant properties; produces amoxapine as an ] ** ] (Loxapac, Loxitane, Adasuve) – a tricyclic ] with antidepressant properties; produces amoxapine as an ]
** ] (Mazanor, Sanorex) ** ] (Mazanor, Sanorex)


Revision as of 04:54, 10 May 2016

Not to be confused with Tetracycline.
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Skeletal formula of tetracyclic antidepressant mirtazapine. Note its four fused "rings".

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:

Pharmacology

Binding profiles

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

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 91 9,400 350 2.0 560
Mianserin 4,000 101 9,400 190 4.3 74 4.3 2,197 1.7 820
Mirtazapine >100,000 1,640 >100,000 ? 69 500 19 >5,454 0.1 670
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. 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)
Antidepressants (N06A)
Specific reuptake inhibitors and/or receptor modulators
SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
Tricyclic and tetracyclic antidepressants
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
Others
Monoamine oxidase inhibitors
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
Adjunctive therapies
Miscellaneous
Acetylcholine receptor modulators
Muscarinic acetylcholine receptor modulators
mAChRsTooltip Muscarinic acetylcholine receptors
Agonists
Antagonists
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Nicotinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators
Nicotinic acetylcholine receptor modulators
nAChRsTooltip Nicotinic acetylcholine receptors
Agonists
(and PAMsTooltip positive allosteric modulators)
Antagonists
(and NAMsTooltip negative allosteric modulators)
Precursors
(and prodrugs)
See also
Receptor/signaling modulators
Muscarinic acetylcholine receptor modulators
Acetylcholine metabolism/transport modulators
Histamine receptor modulators
H1
Agonists
Antagonists
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists
See also
Receptor/signaling modulators
Monoamine metabolism modulators
Monoamine reuptake inhibitors
Serotonin receptor modulators
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Tricyclics
Classes
Antidepressants
(Tricyclic antidepressants (TCAs))
Antihistamines
Antipsychotics
Anticonvulsants
Anticholinergics
Others
Category: