Clinical data
AHFS/Drugs.com International Drug Names
Routes of
ATC code none
Legal status
Legal status
  • Rx-only (JP)
Pharmacokinetic data
Metabolism Hepatic
Excretion Renal
CAS Number 749-02-0 YesY
PubChem (CID) 5265
ChemSpider 5075 YesY
KEGG D01051 YesY
ECHA InfoCard 100.010.931
Chemical and physical data
Formula C23H26FN3O2
Molar mass 395.47 g/mol
3D model (Jmol) Interactive image

Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class.[1] It is licensed for clinical use in Japan as a treatment for schizophrenia.[2] Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl channels (CaCCs), thus a potential target for therapy of cystic fibrosis.[3]

Receptor Ki (nM)[4] Notes
5-HT1A 17.3
5-HT1B 995
5-HT1D 2397
5-HT1E 5051
5-HT1F 3.98
5-HT2A 1.17
5-HT2B 1114.2
5-HT2C 922.9
5-HT3 >10000 No data available from
cloned human receptors.
Data comes from rat cortex
receptors and other sources.
5-HT5A 2512 Cloned mouse receptor.
5-HT6 1590 Cloned rat receptor.
5-HT7 109.8
α1A 20.4
α1B 3.09
α1D 8.32
D1 398.5
D2 0.16
D3 0.34
D4 1.39
D5 4500
H1 272
σ 353

N-Methylspiperone (NMSP) is a derivate of spiperone that is used to study the dopamine and serotonin neurotransmitter system. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography.[5]


  1. Zheng LT, Hwang J, Ock J, Lee MG, Lee WH, Suk K (September 2008). "The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production". J. Neurochem. 107 (5): 1225–35. doi:10.1111/j.1471-4159.2008.05675.x. PMID 18786164.
  2. Mirtazapine. Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 12 September 2011. Retrieved 4 November 2013.
  3. Liang L, Macdonald KD, Schwiebert EM, Zeitlin PL, Guggino WB (October 2008). "Spiperone, Identified through Compound Screening, Activates Calcium Dependent Chloride Secretion in the Airway". Am J Physiol Cell Physiol. 296 (1): C131–41. doi:10.1152/ajpcell.00346.2008. PMID 18987251.
  4. 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. Retrieved 4 November 2013.
  5. Bengt Andree; et al. (August 1998). "Positron Emission Tomographic Analysis of Dose-dependent MDL-100,907 Binding to 5-Hydroxtryptamine-2A Receptors in the Human Brain". Journal of Clinical Psychopharmacology. 18 (4): 313323.
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