Spiperone
From Wikipedia, the free encyclopedia
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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CAS Number | 749-02-0 |
PubChem (CID) | 5265 |
IUPHAR/BPS | 99 |
ChemSpider | 5075 |
UNII | 4X6E73CJ0Q |
KEGG | D01051 |
ChEBI | CHEBI:9233 |
ChEMBL | CHEMBL267930 |
ECHA InfoCard | 100.010.931 |
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.