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]
^Zheng LT, Hwang J, Ock J, Lee MG, Lee WH, Suk K (December 2008). "The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production". Journal of Neurochemistry. 107 (5): 1225–1235. doi:10.1111/j.1471-4159.2008.05675.x. PMID 18786164.
^"Mirtazapine". Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 12 September 2011. Retrieved 4 November 2013.
^Liang L, MacDonald K, Schwiebert EM, Zeitlin PL, Guggino WB (January 2009). "Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway". American Journal of Physiology. Cell Physiology. 296 (1): C131–C141. doi:10.1152/ajpcell.00346.2008. PMC 4116347. PMID 18987251.
^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 4 November 2013.
^Andrée B, Nyberg S, Ito H, Ginovart N, Brunner F, Jaquet F, et al. (August 1998). "Positron emission tomographic analysis of dose-dependent MDL 100,907 binding to 5-hydroxytryptamine-2A receptors in the human brain". Journal of Clinical Psychopharmacology. 18 (4): 317–323. doi:10.1097/00004714-199808000-00012. PMID 9690698.
Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class....
featuring the 4-imidazolidinone ring include hetacillin, NNC 63-0532, spiperone, and spiroxatrine. Imidazolones (also called imidazolinones) are oxo derivatives...
Pimozide binds D2 and D3 with high affinity, also binds D4 receptors Spiperone binds D2, D3 and D4 with high affinity; can also bind D1 Sulpiride binds...