Tiospirone

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Tiospirone
File:Tiospirone.png
Systematic (IUPAC) name
8-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • Uncontrolled
Pharmacokinetic data
Metabolism Hepatic
Biological half-life 1.4 hours
Excretion Urine
Identifiers
CAS Number 87691-91-6
ATC code none
PubChem CID 55752
IUPHAR/BPS 101
ChemSpider 50348
Chemical data
Formula C24H32N4O2S
Molar mass 440.60 g/mol[[Script error: No such module "String".]]
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Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic drug of the azapirone class.[1] It 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.[2][3][4][5][6][7]

Tiospirone was tested in clinical trials for the treatment of schizophrenia in the late 1980s, and was found to have efficacy equivalent to that of typical antipsychotics without causing extrapyramidal side effects.[8][9][10][11] However, development was not continued and it was never marketed.

Perospirone, another azapirone derivative with antipsychotic properties, was synthesized and assayed several years after tiospirone.[12] It was found to be both more potent and more selective in comparison and was commercialized instead.[12]

See also

References

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  10. 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): 190–3. PMID 2574893. 
  11. Nasrallah, Henry A.; Shriqui, Christian L (1995). Contemporary issues in the treatment of schizophrenia. Washington, DC: American Psychiatric Press. p. 313. ISBN 0-88048-681-3.  More than one of |pages= and |page= specified (help)
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