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'''Tetracyclic antidepressants''' ('''TeCAs''') are a ] of ] ]s. They are named after their ], which contains four ]s. They are closely related to the ]s (TCAs). The TeCAs have also been used for the ] of a number of other ]s, including loss of ] or ], ], ], and ] and ], among others. '''Tetracyclic antidepressants''' ('''TeCAs''') are a ] of ] ]s. They are named after their ], which contains four ]s. The TeCAs have also been used for the ] of a number of other ]s, including loss of ] or ], ], ], and ] and ], among others.

They are closely related to the ]s (TCAs).


== List of TeCAs == == List of TeCAs ==

Revision as of 23:15, 7 August 2009

There are also several chemically unrelated tetracyclic antibiotics based on tetracycline.

Chemical structure of the tetracyclic antidepressant mirtazapine.

Tetracyclic antidepressants (TeCAs) are a class of antidepressant drugs. They are named after their chemical structure, which contains four rings of atoms. The TeCAs have also been used for the treatment of a number of other disorders, including loss of appetite or anorexia, anxiety disorders, insomnia, and nausea and vomiting, among others.

They are closely related to the tricyclic antidepressants (TCAs).

List of TeCAs

Pharmacology

Binding Profiles

A number of TeCAs have been compared below:Cite error: The <ref> tag has too many names (see the help page).

Compound SERT NET DAT H1 M1-5 α1 α2 5-HT1A 5-HT2 D2
Amoxapine 58 16 4,310 25 1,000 50 2,600 ? ? ?
Maprotiline 5,800 11.1 1,000 2 570 90 9,400 ? ? ?
Mianserin 4,000 71 9,400 ? ? ? ? ? ? ?
Mirtazapine >1,500 ~1,250 >1,500 ~0.75 ~1,000 ~500 ~100 >1,500 ~10 >1,500
Oxaprotiline 3,900 4.9 4,340 ? ? ? ? ? ? ?
Setiptiline ? ? ? ? ? ? ? ? ? ?

They function as antagonists at all sites listed. Though not shown, amoxapine, mianserin, and mirtazapine are also potent 5-HT3 receptor antagonists.

The values above are expressed as equilibrium dissociation constants. It should be noted that less is more. SERT, NET, and DAT correspond to the abilities of the compounds to inhibit the reuptake of serotonin, norepinephrine, and dopamine, respectively. The other values correspond to their affinity for various receptors.

References

  1. Tatsumi M, Groshan K, Blakely RD, Richelson E. (1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". Eur J Pharmacol. 340 (2–3): 249–258. PMID 9537821.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  2. Owens MJ, Morgan WN, Plott SJ, Nemeroff CB. (1997). "Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites". J Pharmacol Exp Ther. 283 (3): 1305–1322. PMID 9400006.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  3. Cusack B, Nelson A, Richelson E. (1994). "Binding of antidepressants to human brain receptors: focus on newer generation compounds". Psychopharmacology (Berl). 114 (4): 559–565. PMID 7855217.{{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
Anxiolytics (N05B)
5-HT1ARTooltip 5-HT1A receptor agonists
GABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulators
Hypnotics
Gabapentinoids
(α2δ VDCC blockers)
Antidepressants
Antipsychotics
Sympatholytics
(Antiadrenergics)
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5-HT3 serotonin ion
channel antagonists
5-HT serotonin G-protein
receptor antagonists
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(cannabinoids)
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(antihistamines)
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(anticholinergics)
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GABAA
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GABAB
H1
Antihistamines
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5-HT2A
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α2δ VDCC
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Adrenergic receptor modulators
α1
Agonists
Antagonists
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Agonists
Antagonists
β
Agonists
Antagonists
Dopamine receptor modulators
D1-like
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PAMs
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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
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