Tetraciklični antidepresiv

Izvor: Wikipedia
Hemijska struktura tetracikličnog antidepresiva amoksapina

Tetraciklični antidepresivi (TeCA) su klasa lekova koja se prvenstveno koristi kao antidepresivi. Oni su uvedeni u upotrebu tokom 1970-tih. Njihovo ime je proisteklo iz njihove hemijske strukture koja sadrži četiri prstena i koja je blisko srodna sa tricikličnim antidepresivima (TCA) koji sadrže tri prstena.

Farmakologija[uredi - уреди]

Profil vezivanja[uredi - уреди]

Afiniteti (Kd (nM)) selekcije TeCA lekova su upoređeni na nekoliko tipova mesta vezivanja:[1][2][3][4][5][6][7][8]

Jedinjenje SERT NET DAT 5-HT1A 5-HT2A α1 α2 D2 H1 mACh
Amoksapin 58 16.0 4,310 220 0.6 50 2,600 160 25 1,000
Loksapin 2,400 380 9,000 2,900 1.7 28 2,400 70 4.9 450
Maprotilin 5,800 11.1 1,000 12,000 120 90 9,400 350 2.0 570
Mianserin 4,000 101 9,400 190 4.3 74 4.3 2,197 1.7 820
Mirtazapin >100,000 1,640 >100,000  ? 69 608 19 >5,454 1.6 794
Oksaprotilin 3,900 4.9 4,340 67,000 2,400 620 42,000  ? 21 2,900

Izabrani ligandi deluju kao antagonisti (ili inverzni agonisti u zavisnosti od aktivnog mesta) na navedenim receptorima i kao inhibitori transportera.

Reference[uredi - уреди]

  1. Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology 340 (2–3): 249–58. doi:10.1016/S0014-2999(97)01393-9. PMID 9537821. 
  2. Wander TJ, Nelson A, Okazaki H, Richelson E (December 1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro". European Journal of Pharmacology 132 (2–3): 115–21. doi:10.1016/0014-2999(86)90596-0. PMID 3816971. 
  3. 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. 
  4. Tatsumi M, Jansen K, Blakely RD, Richelson E (March 1999). "Pharmacological profile of neuroleptics at human monoamine transporters". European Journal of Pharmacology 368 (2–3): 277–83. doi:10.1016/S0014-2999(99)00005-9. PMID 10193665. 
  5. Wander TJ, Nelson A, Okazaki H, Richelson E (November 1987). "Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro". European Journal of Pharmacology 143 (2): 279–82. doi:10.1016/0014-2999(87)90544-9. PMID 2891550. 
  6. Richelson E, Nelson A (August 1984). "Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro". European Journal of Pharmacology 103 (3–4): 197–204. doi:10.1016/0014-2999(84)90478-3. PMID 6149136. 
  7. Fernández J, Alonso JM, Andrés JI, et al. (March 2005). "Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents". Journal of Medicinal Chemistry 48 (6): 1709–12. doi:10.1021/jm049632c. PMID 15771415. 
  8. de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM (April 1988). "Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers". Neuropharmacology 27 (4): 399–408. doi:10.1016/0028-3908(88)90149-9. PMID 3419539. 

Vidi još[uredi - уреди]