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Systematic (IUPAC) name
CAS number 749-02-0
ATC code none
PubChem 5265
Chemical data
Formula C23H26FN3O2 
Mol. mass 395.47 g/mol
Pharmacokinetic data
Metabolism Hepatic
Excretion Renal
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral
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Spiperone (Spiroperidol, Spiropitan) is a psychoactive drug and research chemical belonging to the butyrophenone chemical class.[1] It functions as a 5-HT1A, 5-HT2A, 5-HT7, and D2 receptor antagonist, and has been used to identify these receptors when labeled with tritium. It has negligible affinity for the 5-HT2C receptor. 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.[2]

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.[3]


  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.. doi:10.1111/j.1471-4159.2008.05675.x. PMID 18786164. 
  2. ^ 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. doi:10.1152/ajpcell.00346.2008. PMID 18987251. 
  3. ^ Bengt Andree and others (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 Psychophamarcology 18 (4): 313–323. 


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