Tetraciklični antidepresiv
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
уредиProfil vezivanja
уредиAfiniteti (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
уреди- ^ Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). „Pharmacological profile of antidepressants and related compounds at human monoamine transporters”. European Journal of Pharmacology. 340 (2–3): 249—58. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9.
- ^ Wander TJ, Nelson A, Okazaki H, Richelson E (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. PMID 3816971. doi:10.1016/0014-2999(86)90596-0.
- ^ Richelson E, Nelson A (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. Архивирано из оригинала 28. 08. 2021. г. Приступљено 21. 09. 2012.
- ^ Tatsumi M, Jansen K, Blakely RD, Richelson E (1999). „Pharmacological profile of neuroleptics at human monoamine transporters”. European Journal of Pharmacology. 368 (2–3): 277—83. PMID 10193665. doi:10.1016/S0014-2999(99)00005-9.
- ^ Wander TJ, Nelson A, Okazaki H, Richelson E (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. PMID 2891550. doi:10.1016/0014-2999(87)90544-9.
- ^ Richelson E, Nelson A (1984). „Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro”. European Journal of Pharmacology. 103 (3–4): 197—204. PMID 6149136. doi:10.1016/0014-2999(84)90478-3.
- ^ Fernández J; Alonso JM; Andrés JI; et al. (2005). „Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents”. Journal of Medicinal Chemistry. 48 (6): 1709—12. PMID 15771415. doi:10.1021/jm049632c.
- ^ de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM (1988). „Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers”. Neuropharmacology. 27 (4): 399—408. PMID 3419539. doi:10.1016/0028-3908(88)90149-9.