Spiperone
From Wikipedia, the free encyclopedia
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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration |
Oral |
| ATC code | none |
| Legal status | |
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| Pharmacokinetic data | |
| Metabolism | Hepatic |
| Excretion | Renal |
| Identifiers | |
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Systematic (IUPAC) name: 8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
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| CAS Number | 749-02-0  |
| PubChem (CID) | 5265 |
| IUPHAR/BPS | 99 |
| ChemSpider | 5075 |
| UNII | 4X6E73CJ0Q |
| KEGG | D01051 |
| ChEBI | CHEBI:9233 |
| ChEMBL | CHEMBL267930 |
| Chemical and physical data | |
| Formula | C23H26FN3O2 |
| Molar mass | 395.47 g/mol |
| 3D model (Jmol) | Interactive image |
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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]
References[edit]
- ^ 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.
- ^ Mirtazapine. Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 12 September 2011. Retrieved 4 November 2013.
- ^ 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.
- ^ 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.
- ^ 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): 313–323.
