Tiospirone

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Tiospirone
Clinical data
ATC code
  • none
Legal status
Legal status
  • Development terminated
Pharmacokinetic data
MetabolismHepatic
Elimination half-life1.4 hours
ExcretionUrine
Identifiers
  • 8-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H32N4O2S
Molar mass440.61 g·mol−1

Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an

potent and more selective in comparison and was commercialized instead.[6]

Pharmacology

Pharmacodynamics

Tiospirone acts as a

D4, and α1-adrenergic receptor antagonist.[7][8][9][10][11][12]

Binding profile[13]

Receptor Ki (nM)
5-HT2A 0.06
5-HT2C 9.73
5-HT6 950
5-HT7 0.64
M1 630
M2 180
M3 1290
M4 480
M5 3900
D2 0.5
D4 13.6

See also

References

  1. PMID 2869146
    .
  2. PMID 2885367
    .
  3. PMID 3294920
    .
  4. PMID 2574893
    .
  5. ISBN 0-88048-681-3
    .
  6. ^
    PMID 8582016
    .
  7. PMID 7766287
    .
  8. S2CID 13549491
    .
  9. PMID 11561089
    .
  10. PMID 10991983
    .
  11. S2CID 29337002
    .
  12. S2CID 36271263
    .
  13. ^ Roth BL, Driscol J (12 January 2011). "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Archived from the original on 8 November 2013. Retrieved 3 December 2013.