Tiospirone(BMY-13,859), also sometimes calledtiaspironeortiosperone,is anatypical antipsychoticof theazapironeclass.[1]It was investigated as a treatment forschizophreniain the late 1980s and was found to have an effectiveness equivalent to those oftypical antipsychoticsinclinical trialsbut without causingextrapyramidalside 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 morepotentand moreselectivein comparison and was commercialized instead.[6]
^Yevich JP, New JS, Smith DW, Lobeck WG, Catt JD, Minielli JL, et al. (March 1986). "Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents".Journal of Medicinal Chemistry.29(3): 359–369.doi:10.1021/jm00153a010.PMID2869146.
^Jain AK, Kelwala S, Moore N, Gershon S (April 1987). "A controlled clinical trial of tiaspirone in schizophrenia".International Clinical Psychopharmacology.2(2): 129–133.doi:10.1097/00004850-198704000-00006.PMID2885367.
^Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S (April 1987). "Tiaspirone in schizophrenia".Journal of Clinical Psychopharmacology.7(2): 98–101.doi:10.1097/00004714-198704000-00010.PMID3294920.
^Borison RL, Sinha D, Haverstock S, McLarnon MC, Diamond BI (1989). "Efficacy and safety of tiospirone vs. haloperidol and thioridazine in a double-blind, placebo-controlled trial".Psychopharmacology Bulletin.25(2): 190–193.PMID2574893.
^Sumiyoshi T, Suzuki K, Sakamoto H, Yamaguchi N, Mori H, Shiba K, Yokogawa K (February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy".Neuropsychopharmacology.12(1): 57–64.doi:10.1016/0893-133X(94)00064-7.PMID7766287.
^Roth BL,Tandra S, Burgess LH, Sibley DR, Meltzer HY (August 1995). "D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs".Psychopharmacology.120(3): 365–368.doi:10.1007/BF02311185.PMID8524985.S2CID13549491.
^Rauly-Lestienne I, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Cussac D (October 2007). "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".Naunyn-Schmiedeberg's Archives of Pharmacology.376(1–2): 93–105.doi:10.1007/s00210-007-0182-6.PMID17786406.S2CID29337002.
^Newman-Tancredi A, Assié MB, Leduc N, Ormière AM, Danty N, Cosi C (September 2005). "Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia".The International Journal of Neuropsychopharmacology.8(3): 341–356.doi:10.1017/S1461145704005000.PMID15707540.S2CID36271263.
^Roth BL, Driscol J (12 January 2011)."PDSP KiDatabase ".Psychoactive Drug Screening Program (PDSP).University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Archived fromthe originalon 8 November 2013.Retrieved3 December2013.
