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Revision as of 02:05, 3 June 2009 by Vanished 45kd09la13 (talk | contribs) (→Comparison)(diff) ← Previous revision | Latest revision (diff) | Newer revision → (diff)There are also several chemically unrelated tetracyclic antibiotics based on Tetracycline.
Tetracyclic antidepressants (TeCAs) are a class of antidepressant drugs. They are named after their molecular structure, which contains four rings of atoms. They are closely related to the tricyclic antidepressants (TCAs). The TeCAs have also been used for the treatment of a number of other disorders, including anorexia, anxiety disorders, insomnia, and nausea/emesis, among others.
List of TeCAs
- Pharmaceuticals
- Amoxapine (Asendin, Asendis, Defanyl, Demolox, Moxadil)
- Maprotiline (Deprilept, Ludiomil, Psymion)
- Mianserin (Tolvon)
- Mirtazapine (Remeron, Remergil, Zispin, Avanza)
- Research Chemicals
Comparison
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 | 1~ | 1,000~ | 500~ | 100~ | >1,500 | 10~ | >1,500 |
| Oxaprotiline | 3,900 | 4.9 | 4,340 | ? | ? | ? | ? | ? | ? | ? |
They function as antagonist at all sites. 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
- 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) - 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) - 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)