Tetraciklični antidepresiv

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

Profil vezivanja

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

Jedinjenje	SERT	NET	DAT	5-HT_1A	5-HT_2A	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

↑ 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.
↑ 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.
↑ 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. Arhivirano iz originala na datum 2021-08-28. Pristupljeno 2014-03-13.
↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Povezano

Triciklični antidepresivi (TCA)

[pmid9537821-1] 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.

[pmid3816971-2] 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.

[pmid6086881-3] 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. Arhivirano iz originala na datum 2021-08-28. Pristupljeno 2014-03-13.

[pmid10193665-4] 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.

[pmid2891550-5] 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.

[pmid6149136-6] 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.

[pmid15771415-7] 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.

[pmid3419539-8] 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.

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