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Spiperone

Chemical compound

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Spiperone, also known as spiroperidol and sold under the brand name Spiropitan ((JP)) is a typical antipsychotic of the butyrophenone family related to haloperidol. It is approved for clinical use in Japan as a treatment for schizophrenia.

Pharmacology

Pharmacodynamics

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	vauthors = Bender AM, Parr LC, Livingston WB, Lindsley CW, Merryman WD	title = 2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery	journal = J Med Chem	volume = 66	issue = 16	pages = 11027–11039	date = August 2023	pmid = 37584406	pmc = 11073569	doi = 10.1021/acs.jmedchem.3c01178	url = }}
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.

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.

Chemistry

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.

References

(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.
(12 September 2011). "Martindale: The Complete Drug Reference". The Royal Pharmaceutical Society of Great Britain.
(12 January 2011). "PDSP K_i Database". University of North Carolina at Chapel Hill and the United States National Institute of Mental Health.
(August 2023). "2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery". J Med Chem.
(January 1987). "Central serotonin receptors as targets for drug research". J Med Chem.
Janssen, P.A.J.. (1982). "Biochemical Immunological Pharmacology". Elsevier.
(January 2009). "Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway". American Journal of Physiology. Cell Physiology.
(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.

Info: Wikipedia Source

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5-ht2a-antagonists alpha-1-blockers butyrophenone-antipsychotics d2-antagonists 4-fluorophenyl-compounds imidazolidinones spiro-compounds typical-antipsychotics

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