| 词条 | Cyanodothiepin |
| 释义 |
| IUPAC_name = 11-(3-(dimethylamino)propylidene)-6,11-dihydrodibenzo[b,e]thiepine-2-carbonitrile | image = Cyanodothiepin.svg | CAS_number = 90667-37-1 | ATC_prefix = None | ATC_suffix = | PubChem = 13276753 | C=20 | H=20 | N=2 | S=1 | molecular_weight = 320.45 g/mol | SMILES = CN(C)CC/C=C1C2=C(C=CC(C#N)=C2)SCC3=C/1C=CC=C3 | ChemSpiderID = 30780728 | StdInChI = 1S/C20H20N2S/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-23-20-10-9-15(13-21)12-19(18)20/h3-4,6-10,12H,5,11,14H2,1-2H3/b18-8+ | StdInChIKey = FSIRGTNPQFDCCD-QGMBQPNBSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_category = | legal_status = | routes_of_administration = | synonyms = BTS-56424 }}Cyanodothiepin (developmental code name BTS-56424) is a tricyclic antidepressant (TCA) acting as a potent and highly selective (over norepinephrine and dopamine uptake) inhibitor of the reuptake of serotonin that was never marketed.[1][2][3] It also has moderate affinity for the muscarinic acetylcholine receptors and weak/negligible affinity for the α1-adrenergic, 5-HT2A, D1, and D2 receptors;[1][2][3] the H1 receptor has not been assayed,[3] but cyanodothiepin is less sedating than the related drug cianopramine, suggesting that its antihistamine activity is not as pronounced as other TCAs.[1][3] Cyanodothiepin is active in the forced swimming test (FST), implying that it may possess antidepressant properties in humans. However, it is only weakly active compared to cianopramine and imipramine in monoamine depletion-based tests of antidepressant potential.[1] See also
References1. ^1 2 3 {{ cite journal |author1=Luscombe, G. P. |author2=Buckett, W. R. | title = Pharmacology of Cyanodothiepin (BTS 56 424), a Selective 5-Hydroxytryptamine Reuptake Inhibitor | journal = Drug Development Research | volume = 29 | issue = 3 | pages = 235–248 | year = 1993 | pmid = | doi = 10.1002/ddr.430290311 }} {{Antidepressants}}{{Navboxes2. ^1 {{ cite book | author = Jucker, E. | title = Progress in Drug Research | url = https://books.google.com/books?id=gwhdUGoO6KwC&pg=PA80 | accessdate = 2011-11-25 | year = 2000 | publisher = Birkhäuser | isbn = 978-3-7643-6113-6 | pages = 79–80 }} 3. ^1 2 3 {{ cite book | author1 = Olivier, B. | author2 = van Wijngaarden, I. | author3 = Soudijn, W. | title = Serotonin Receptors and their Ligands | url = https://books.google.com/books?id=lfo0hGqIex0C&pg=PA332 | accessdate = 2011-11-25 | year = 1997 | publisher = Elsevier | isbn = 978-0-444-82041-9 | page = 332 }} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Histamine receptor modulators}}{{Monoamine reuptake inhibitors}}{{Muscarinic acetylcholine receptor modulators}}{{Serotonin receptor modulators}} }}{{Tricyclics}}{{Nervous-system-drug-stub}} 8 : Amines|Antihistamines|Dibenzothiepines|H1 receptor antagonists|Muscarinic antagonists|Nitriles|Selective serotonin reuptake inhibitors|Tricyclic antidepressants |
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