Tetracyclic antidepressant

From Infogalactic: the planetary knowledge core
Jump to: navigation, search
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:[1][2][3][4][5][6][7][8][9]

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.

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.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  2. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  3. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  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.<templatestyles src="Module:Citation/CS1/styles.css"></templatestyles>
  5. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  6. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  7. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  8. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).
  9. Lua error in Module:Citation/CS1/Identifiers at line 47: attempt to index field 'wikibase' (a nil value).