Tetracyclic antidepressant

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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. 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 loss of appetite or anorexia, anxiety disorders, insomnia, and nausea and vomiting, among others.

Contents

[edit] List of TeCAs

[edit] Pharmacology

[edit] Binding Profiles

A number of TeCAs have been compared below:[1][2][3][4]

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.

[edit] 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. 
  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. 
  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. 
  4. ^ Alan F. Schatzberg, Charles B. (2006). Essentials of clinical psychopharmacology. American Psychiatric Pub. p. 7. ISBN 1585622435, 9781585622436. 


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