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{{Distinguish|Tetracycline}} |
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{{Distinguish|Tetracycline}} |
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] of the tetracyclic antidepressant ]. Notice its four fused ]s.]] |
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] of the tetracyclic antidepressant ]. Notice its four fused ]s.]] |
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{{Refimprove|date=November 2013}} |
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'''Tetracyclic antidepressants''' ('''TeCAs''') are a class of ]s that were first introduced in the 1970s. They are named after their ] which contains four ]s, and are closely related to the ]s (TCAs), which contain three rings of atoms. |
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{{refimprove|date=November 2013}} |
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'''Tetracyclic antidepressants''' ('''TeCAs''') are a ] of ]s used primarily as ]s that were first introduced in the 1970s. They are named after their ] which contains four ]s and are closely related to the ]s (TCAs) which contain three rings of atoms. |
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== List of TeCAs == |
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==List of TeCAs== |
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The TeCAs include the following agents: |
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The TeCAs include the following agents: |
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* Marketed |
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* Pharmaceutical drugs |
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** ] (Asendin) — sometimes classed as a secondary amine tricyclic antidepressant; active metabolite of the typical antipsychotic, ]. |
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** ] (Asendin) — sometimes classed as a secondary amine tricyclic antidepressant; active metabolite of the typical antipsychotic, ]. |
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** ] (Deprilept, Ludiomil, Psymion) |
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** ] (Deprilept, Ludiomil, Psymion) |
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** ] (Remeron, Avanza, Zispin) |
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** ] (Remeron, Avanza, Zispin) |
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** ] (Tecipul) |
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** ] (Tecipul) |
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* Not marketed |
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* Research chemicals |
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** ] (CGS-7525A) |
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** ] (CGS-7525A) |
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** ] (WY-23,409) |
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** ] (WY-23,409) |
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** ] (ORG-50,081) |
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** ] (ORG-50,081) |
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** ] |
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** ] |
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** ] (SCA-136) is a selective 5-HT<sub>2C</sub> full agonist that was being investigated as an antidepressant and ] and was later dropped by its developer, ]. |
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== Pharmacology == |
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=== Binding profiles === |
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==Pharmacology== |
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===Binding profiles=== |
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The ] (K<sub>d</sub> (nM)) of a selection of TeCAs have been compared below at an assortment of ]s:<ref name=Goodman>{{cite book|last=Brunton|first=Laurence|title=Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th Edition|year=2011|publisher=McGraw-Hill|location=China|isbn=978-0-07-162442-8|pages=406-410}}</ref><ref name="pmid9537821">{{cite journal | author = Tatsumi M, Groshan K, Blakely RD, Richelson E | title = Pharmacological profile of antidepressants and related compounds at human monoamine transporters | journal = European Journal of Pharmacology | volume = 340 | issue = 2–3 | pages = 249–58 |date=December 1997 | pmid = 9537821 | doi = 10.1016/S0014-2999(97)01393-9| url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(97)01393-9}}</ref><ref name="pmid3816971">{{cite journal | author = Wander TJ, Nelson A, Okazaki H, Richelson E | title = Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 132 | issue = 2–3 | pages = 115–21 |date=December 1986 | pmid = 3816971 | doi = 10.1016/0014-2999(86)90596-0| url = }}</ref><ref name="pmid6086881">{{cite journal | author = Richelson E, Nelson A | title = Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 230 | issue = 1 | pages = 94–102 |date=July 1984 | pmid = 6086881 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6086881}}</ref><ref name="pmid10193665">{{cite journal | author = Tatsumi M, Jansen K, Blakely RD, Richelson E | title = Pharmacological profile of neuroleptics at human monoamine transporters | journal = European Journal of Pharmacology | volume = 368 | issue = 2–3 | pages = 277–83 |date=March 1999 | pmid = 10193665 | doi = 10.1016/S0014-2999(99)00005-9| url = }}</ref><ref name="pmid2891550">{{cite journal | author = Wander TJ, Nelson A, Okazaki H, Richelson E | title = Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 143 | issue = 2 | pages = 279–82 |date=November 1987 | pmid = 2891550 | doi = 10.1016/0014-2999(87)90544-9| url = http://linkinghub.elsevier.com/retrieve/pii/0014-2999(87)90544-9}}</ref><ref name="pmid6149136">{{cite journal | author = Richelson E, Nelson A | title = Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 103 | issue = 3–4 | pages = 197–204 |date=August 1984 | pmid = 6149136 | doi = 10.1016/0014-2999(84)90478-3| url = }}</ref><ref name="pmid15771415">{{cite journal | author = Fernández J, Alonso JM, Andrés JI, ''et al.'' | title = Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents | journal = Journal of Medicinal Chemistry | volume = 48 | issue = 6 | pages = 1709–12 |date=March 2005 | pmid = 15771415 | doi = 10.1021/jm049632c}}</ref><ref name="pmid3419539">{{cite journal | author = de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM | title = Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers | journal = Neuropharmacology | volume = 27 | issue = 4 | pages = 399–408 |date=April 1988 | pmid = 3419539 | doi = 10.1016/0028-3908(88)90149-9| url = }}</ref> |
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The ] (K<sub>d</sub> (nM)) of a selection of TeCAs have been compared below at an assortment of ]s:<ref name=Goodman>{{cite book|last=Brunton|first=Laurence|title=Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th Edition|year=2011|publisher=McGraw-Hill|location=China|isbn=978-0-07-162442-8|pages=406-410}}</ref><ref name="pmid9537821">{{cite journal | author = Tatsumi M, Groshan K, Blakely RD, Richelson E | title = Pharmacological profile of antidepressants and related compounds at human monoamine transporters | journal = European Journal of Pharmacology | volume = 340 | issue = 2–3 | pages = 249–58 |date=December 1997 | pmid = 9537821 | doi = 10.1016/S0014-2999(97)01393-9| url = http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(97)01393-9}}</ref><ref name="pmid3816971">{{cite journal | author = Wander TJ, Nelson A, Okazaki H, Richelson E | title = Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 132 | issue = 2–3 | pages = 115–21 |date=December 1986 | pmid = 3816971 | doi = 10.1016/0014-2999(86)90596-0| url = }}</ref><ref name="pmid6086881">{{cite journal | author = Richelson E, Nelson A | title = Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 230 | issue = 1 | pages = 94–102 |date=July 1984 | pmid = 6086881 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=6086881}}</ref><ref name="pmid10193665">{{cite journal | author = Tatsumi M, Jansen K, Blakely RD, Richelson E | title = Pharmacological profile of neuroleptics at human monoamine transporters | journal = European Journal of Pharmacology | volume = 368 | issue = 2–3 | pages = 277–83 |date=March 1999 | pmid = 10193665 | doi = 10.1016/S0014-2999(99)00005-9| url = }}</ref><ref name="pmid2891550">{{cite journal | author = Wander TJ, Nelson A, Okazaki H, Richelson E | title = Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 143 | issue = 2 | pages = 279–82 |date=November 1987 | pmid = 2891550 | doi = 10.1016/0014-2999(87)90544-9| url = http://linkinghub.elsevier.com/retrieve/pii/0014-2999(87)90544-9}}</ref><ref name="pmid6149136">{{cite journal | author = Richelson E, Nelson A | title = Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro | journal = European Journal of Pharmacology | volume = 103 | issue = 3–4 | pages = 197–204 |date=August 1984 | pmid = 6149136 | doi = 10.1016/0014-2999(84)90478-3| url = }}</ref><ref name="pmid15771415">{{cite journal | author = Fernández J, Alonso JM, Andrés JI, ''et al.'' | title = Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents | journal = Journal of Medicinal Chemistry | volume = 48 | issue = 6 | pages = 1709–12 |date=March 2005 | pmid = 15771415 | doi = 10.1021/jm049632c}}</ref><ref name="pmid3419539">{{cite journal | author = de Boer TH, Maura G, Raiteri M, de Vos CJ, Wieringa J, Pinder RM | title = Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers | journal = Neuropharmacology | volume = 27 | issue = 4 | pages = 399–408 |date=April 1988 | pmid = 3419539 | doi = 10.1016/0028-3908(88)90149-9| url = }}</ref> |
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The selected ligands act as ]s (or ]s depending on the site in question) at all ]s listed and as ]s of all ]s listed. |
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The selected ligands act as ]s (or ]s depending on the site in question) at all ]s listed and as ]s of all ]s listed. |
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== See also == |
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==References== |
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* ] (TCA) |
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== References == |
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{{Reflist|2}} |
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{{Reflist|2}} |
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