| 词条 | Setiptiline | ||||||||||||||||||||||||||||||||||||||||||||||||
| 释义 |
| Verifiedfields = changed | verifiedrevid = 464389691 | IUPAC_name = 2-methyl-2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine | image = Setiptiline 2D structure.svg | width = 200px | tradename = Tecipul | Drugs.com = {{drugs.com|international|setiptiline}} | pregnancy_category = | legal_status = Rx-only | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 57262-94-9 | ATC_prefix = none | ATC_suffix = | ATC_supplemental = | PubChem = 5205 | DrugBank_Ref = {{drugbankcite|changed|drugbank}} | DrugBank = DB09304 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 5016 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 7L38105Z6E | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08511 | synonyms = Teciptiline; delta(13b,4a),4a-Carba-mianserin; MO-8282; ORG-8282 | C=19 | H=19 | N=1 | molecular_weight = 261.36 g/mol | SMILES = c42c(\\C3=C(/c1ccccc1C2)CN(C)CC3)cccc4 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C19H19N/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20/h2-9H,10-13H2,1H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = GVPIXRLYKVFFMK-UHFFFAOYSA-N }}Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida.[1][2] PharmacologyPharmacodynamics{{See also|Pharmacology of antidepressants|Tetracyclic antidepressant#Binding profiles}}
Setiptiline acts as a norepinephrine reuptake inhibitor,[4] α2-adrenergic receptor antagonist,[5] and serotonin receptor antagonist,[6] likely at the 5-HT2 subtypes,{{Citation needed|date=September 2017}} as well as an H1 receptor inverse agonist/antihistamine.[4]{{Additional citation needed|date=September 2017}} ChemistrySetiptiline has a tetracyclic structure and is a close analogue of mianserin and mirtazapine, with setiptiline being delta(13b,4a),4a-carba-mianserin, and mirtazapine being 6-azamianserin. See also
References1. ^{{ cite book |author1=Buschmann, H. |author2=Torrens, A. |author3=Vela, J. M. | url = https://books.google.com/books?id=yXD4QA-Y_Z0C&pg=PA248#v=onepage&q=&f=false | title = Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application | volume = 1 | page=248 | publisher= Wiley VCH | year=2007 | isbn=978-3-527-31058-6}} {{Antidepressants}}{{Anxiolytics}}{{Navboxes2. ^{{ cite book | url = https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA942#v=onepage&f=false | title = Index Nominum 2000: International Drug Directory | page = 942 | editor = Swiss Pharmaceutical Society | publisher = Medpharm Scientific Publishers | year = 2000 | isbn = 3-88763-075-0 }} 3. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 14 August 2017 | url = https://kidbdev.med.unc.edu/databases/pdsp.php?knowID=0&kiKey=&receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=setiptiline&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query}} 4. ^1 2 3 4 {{cite journal | vauthors = Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K | title = [Pharmacological properties of MO-8282, a novel antidepressant] | language = Japanese | journal = Nippon Yakurigaku Zasshi | volume = 88 | issue = 4 | pages = 309–20 | year = 1986 | pmid = 3792961 | doi = | url = }} 5. ^1 {{cite journal | vauthors = Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M | title = [Pharmacological studies of MO-8282, a new antidepressant] | language = Japanese | journal = Nippon Yakurigaku Zasshi | volume = 88 | issue = 6 | pages = 457–66 | year = 1986 | pmid = 2881854 | doi = | url = }} 6. ^{{cite journal | vauthors = Przegaliński E, Baran L, Siwanowicz J, Rawłów A | title = The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282 | journal = Pol J Pharmacol Pharm | volume = 38 | issue = 4 | pages = 377–84 | year = 1986 | pmid = 3774630 | doi = | url = }} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Histamine receptor modulators}}{{Monoamine reuptake inhibitors}}{{Serotonin receptor modulators}} }}{{Tricyclics}}{{nervous-system-drug-stub}} 6 : Alpha-2 blockers|H1 receptor antagonists|Noradrenergic and specific serotonergic antidepressants|Piperidines|Serotonin antagonists|Tetracyclic antidepressants |
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