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Wikipedia / Spiperone

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

0.8 is bovine

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 at targets

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.

See also

References