Spiperone Explained
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 |
|---|
| 17.3 | |
| 995 | |
| 2397 | |
| 5051 | |
| 3.98 | |
| 1.17 | |
| 1114.2 | |
| 922.9 | |
| >10000 | No data available from
cloned human receptors.
Data comes from rat cortex
receptors and other sources. |
| 2512 | Cloned mouse receptor. |
| 1590 | Cloned rat receptor. |
| 109.8 | |
| 20.4 | |
| 3.09 | |
| 8.32 | |
| 398.5 | |
| 0.16 | |
| 0.34 | |
| 1.39 | |
| 4500 | |
| 272 | |
| 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]
Notes and References
- Zheng LT, Hwang J, Ock J, Lee MG, Lee WH, Suk K . 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 . December 2008 . 18786164 . 10.1111/j.1471-4159.2008.05675.x . free .
- Book: Mirtazapine . Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 4 November 2013. 12 September 2011. http://www.medicinescomplete.com/mc/martindale/current/11022-r.htm.
- Liang L, MacDonald K, Schwiebert EM, Zeitlin PL, Guggino WB . Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway . American Journal of Physiology. Cell Physiology . 296 . 1 . C131–C141 . January 2009 . 18987251 . 4116347 . 10.1152/ajpcell.00346.2008 .
- Web site: PDSP Ki Database . Psychoactive Drug Screening Program (PDSP) . Roth BL, Driscol J . Bryan Roth . University of North Carolina at Chapel Hill and the United States National Institute of Mental Health . 4 November 2013 . 12 January 2011 . dead . https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php . 8 November 2013 .
- Andrée B, Nyberg S, Ito H, Ginovart N, Brunner F, Jaquet F, Halldin C, Farde L . 6 . 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 . August 1998 . 9690698 . 10.1097/00004714-199808000-00012 .
