Spiperone
Template:Short description Template:Drugbox
Spiperone, also known as spiroperidol and sold under the brand name Spiropitan ((JP)) is a typical antipsychotic of the butyrophenone family related to haloperidol.[1] It is approved for clinical use in Japan as a treatment for schizophrenia.[2]
Pharmacology
| Receptor | Ki (nM) | Notes |
|---|---|---|
| 5-HT1A | 17.3 | |
| 5-HT1B | 995 | |
| 5-HT1D | 2397 | |
| 5-HT1E | 5051 | |
| 5-HT1F | 3.98 | |
| 5-HT2A | 1.17 | |
| 5-HT2B | 0.8–1114.2 | 0.8 is bovine[4] |
| 5-HT2C | 922.9 | |
| 5-HT3 | >10000 | Rat/other |
| 5-HT5A | 2512 | Mouse |
| 5-HT6 | 1590 | Rat |
| 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 |
Spiperone interacts with various monoamine receptors.[5][3]
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.[6]
Derivatives
N-Methylspiperone (NMSP) is a derivative 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.[7]
See also
References
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