| 词条 | Tiospirone | ||||||||||||||||||||||||
| 释义 |
| IUPAC_name = 8-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione | image = Tiospirone.svg | width = 275 | tradename = | pregnancy_category = | legal_status = Development terminated | routes_of_administration = | bioavailability = | metabolism = Hepatic | elimination_half-life = 1.4 hours | excretion = Urine | CAS_number = 87691-91-6 | ATC_prefix = none | ATC_suffix = | PubChem = 55752 | IUPHAR_ligand = 101 | ChemSpiderID = 50348 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 35C6UMO5SR | ChEMBL = 35057 | C = 24 | H = 32 | N = 4 | O = 2 | S = 1 | molecular_weight = 440.60 g/mol }}Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic of the azapirone class.[1] It was investigated as a treatment for schizophrenia in the late 1980s and was found to have an effectiveness equivalent to those of typical antipsychotics in clinical trials but without causing extrapyramidal side effects.[2][3][4][5] However, development was halted and it was not marketed. Perospirone, another azapirone derivative with antipsychotic properties, was synthesized and assayed several years after tiospirone.[6] It was found to be both more potent and more selective in comparison and was commercialized instead.[6] PharmacologyPharmacodynamicsTiospirone acts as a 5-HT1A receptor partial agonist, 5-HT2A, 5-HT2C, and 5-HT7 receptor inverse agonist, and D2, D4, and α1-adrenergic receptor antagonist.[7][8][9][10][11][12] Binding profile[13]
See also
References1. ^{{cite journal |vauthors=Yevich JP, New JS, Smith DW, etal | title = Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents | journal = Journal of Medicinal Chemistry | volume = 29 | issue = 3 | pages = 359–69 |date=March 1986 | pmid = 2869146 | doi = 10.1021/jm00153a010| url = }} {{Antipsychotics}}{{Navboxes2. ^{{cite journal |vauthors=Jain AK, Kelwala S, Moore N, Gershon S | title = A controlled clinical trial of tiaspirone in schizophrenia | journal = International Clinical Psychopharmacology | volume = 2 | issue = 2 | pages = 129–33 |date=April 1987 | pmid = 2885367 | doi = 10.1097/00004850-198704000-00006| url = }} 3. ^{{cite journal |vauthors=Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S | title = Tiaspirone in schizophrenia | journal = Journal of Clinical Psychopharmacology | volume = 7 | issue = 2 | pages = 98–101 |date=April 1987 | pmid = 3294920 | doi = 10.1097/00004714-198704000-00010| url = }} 4. ^{{cite journal |vauthors=Borison RL, Sinha D, Haverstock S, McLarnon MC, Diamond BI | title = Efficacy and safety of tiospirone vs. haloperidol and thioridazine in a double-blind, placebo-controlled trial | journal = Psychopharmacology Bulletin | volume = 25 | issue = 2 | pages = 190–3 | year = 1989 | pmid = 2574893 | doi = | url = }} 5. ^{{cite book |author1=Nasrallah, Henry A. |author2=Shriqui, Christian L | title = Contemporary issues in the treatment of schizophrenia | publisher = American Psychiatric Press | location = Washington, DC | year = 1995 | page = 313 | isbn = 0-88048-681-3 | oclc = | doi = | url = https://books.google.com/books?id=ut79yW-IZx4C&lpg=PA313&dq=tiospirone%20adrenergic&pg=PA313#v=onepage&q=&f=false}} 6. ^1 {{cite journal |vauthors=Ishizumi K, Kojima A, Antoku F, Saji I, Yoshigi M | title = Succinimide derivatives. II. Synthesis and antipsychotic activity of N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis- cyclohexanedicarboximide (SM-9018) and related compounds | journal = Chemical & Pharmaceutical Bulletin | volume = 43 | issue = 12 | pages = 2139–51 |date=December 1995 | pmid = 8582016 | doi = 10.1248/cpb.43.2139| url = }} 7. ^{{cite journal |vauthors=Sumiyoshi T, Suzuki K, Sakamoto H, etal | title = Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy | journal = Neuropsychopharmacology | volume = 12 | issue = 1 | pages = 57–64 |date=February 1995 | pmid = 7766287 | doi = 10.1016/0893-133X(94)00064-7}} 8. ^{{cite journal |vauthors=Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY | title = D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs | journal = Psychopharmacology | volume = 120 | issue = 3 | pages = 365–8 |date=August 1995 | pmid = 8524985 | doi = 10.1007/BF02311185| url = }} 9. ^{{cite journal |vauthors=Weiner DM, Burstein ES, Nash N, etal | title = 5-hydroxytryptamine2A receptor inverse agonists as antipsychotics | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 299 | issue = 1 | pages = 268–76 |date=October 2001 | pmid = 11561089 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=11561089}} 10. ^{{cite journal |vauthors=Herrick-Davis K, Grinde E, Teitler M | title = Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 295 | issue = 1 | pages = 226–32 |date=October 2000 | pmid = 10991983 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=10991983}} 11. ^{{cite journal |vauthors=Rauly-Lestienne I, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Cussac D | title = Differential profile of typical, atypical and third generation antipsychotics at human 5-HT7a receptors coupled to adenylyl cyclase: detection of agonist and inverse agonist properties | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 376 | issue = 1–2 | pages = 93–105 |date=October 2007 | pmid = 17786406 | doi = 10.1007/s00210-007-0182-6 }} 12. ^{{cite journal |vauthors=Newman-Tancredi A, Assié MB, Leduc N, Ormière AM, Danty N, Cosi C | title = Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia | journal = The International Journal of Neuropsychopharmacology | volume = 8 | issue = 3 | pages = 341–56 |date=September 2005 | pmid = 15707540 | doi = 10.1017/S1461145704005000 | url = http://journals.cambridge.org/abstract_S1461145704005000}} 13. ^{{cite web | title = PDSP Ki Database | work = Psychoactive Drug Screening Program (PDSP) | author1 = Roth, BL | author2 = Driscol, J | url = http://pdsp.med.unc.edu/pdsp.php | publisher = University of North Carolina at Chapel Hill and the United States National Institute of Mental Health | accessdate = 3 December 2013 | date = 12 January 2011 | deadurl = yes | archiveurl = https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php | archivedate = 8 November 2013 | df = }} | title = Pharmacodynamics | titlestyle = background:#ccccff | list1 ={{Adrenergic receptor modulators}}{{Dopamine receptor modulators}}{{Serotonin receptor modulators}}{{Sigma receptor modulators}} }} 5 : Abandoned drugs|Antipsychotics|Azapirones|Benzothiazoles|Piperazines |
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