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{{Tricyclics}}




Revision as of 08:06, 12 January 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, which 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

A number of TeCAs have been compared below:

Compound SERT NET DAT H1 M1-5 α1 α2 5-HT1A 5-HT2A 5-HT2C 5-HT3 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 0.40 ? 34 73 190 7 ? ? ?
Mirtazapine >1,500 ~1,250 >1,500 ~0.75 ~1,000 ~500 ~100 >1,500 ~10 ~10 ~10 >1,500
Oxaprotiline 3,900 4.9 4,340 ? ? ? ? ? ? ? ? ?
Setiptiline ? ? ? ? ? ? ? ? ? ? ? ?

They function as antagonists at all sites listed.

The values above are expressed as equilibrium dissociation constants. It should be noted that lower values correspond to higher binding at the site, or in other words, 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.

See also

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. doi:10.1016/S0014-2999(97)01393-9. 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. doi:10.1007/BF02244985. PMID 7855217.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. Alan F. Schatzberg, Charles B. (2006). Essentials of clinical psychopharmacology. American Psychiatric Pub. p. 7. ISBN 1585622435, 9781585622436. {{cite book}}: Check |isbn= value: invalid character (help)
  5. http://www.psychotropical.com/Mirt_medioc_science.shtml


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)
Others
Antipsychotics (N05A)
Typical
Disputed
Atypical
Others
Antiemetics (A04)
5-HT3 serotonin ion
channel antagonists
5-HT serotonin G-protein
receptor antagonists
CB1 agonists
(cannabinoids)
D2/D3 antagonists
H1 antagonists
(antihistamines)
mACh antagonists
(anticholinergics)
NK1 antagonists
Others
Hypnotics/sedatives (N05C)
GABAA
Alcohols
Barbiturates
Benzodiazepines
Carbamates
Imidazoles
Monoureides
Neuroactive steroids
Nonbenzodiazepines
Phenols
Piperidinediones
Quinazolinones
Others
GABAB
H1
Antihistamines
Antidepressants
Antipsychotics
α2-Adrenergic
5-HT2A
Antidepressants
Antipsychotics
Others
Melatonin
Orexin
α2δ VDCC
Others
Adrenergic receptor modulators
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
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
Dopamine receptor modulators
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
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


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