Raclopride

Chemical compound From Wikipedia, the free encyclopedia

Raclopride is a typical antipsychotic. It acts as a selective antagonist on D2 dopamine receptors.[1] It has been used in trials studying Parkinson Disease.[2]

ATC code
  • none
Quick facts Clinical data, ATC code ...
Raclopride
Clinical data
ATC code
  • none
Identifiers
  • 3,5-dichloro-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide
CAS Number
PubChem CID
IUPHAR/BPS
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KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H20Cl2N2O3
Molar mass347.24 g·mol−1
3D model (JSmol)
  • Clc1c(O)c(c(OC)c(Cl)c1)C(=O)NC[C@H]2N(CC)CCC2
  • InChI=1S/C15H20Cl2N2O3/c1-3-19-6-4-5-9(19)8-18-15(21)12-13(20)10(16)7-11(17)14(12)22-2/h7,9,20H,3-6,8H2,1-2H3,(H,18,21)/t9-/m0/s1 checkY
  • Key:WAOQONBSWFLFPE-VIFPVBQESA-N checkY
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Raclopride is selective for D2 and D3 dopamine receptors.[3]

More information Receptor, Ki ...
Binding profile[3]
Receptor Ki
D1 18000 nM
D2 1.8
D3 3.5
D4 2400
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It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for in vitro imaging (autoradiography) as well as in vivo imaging positron emission tomography (PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the diagnosis of movement disorders. In particular, cerebral D2 receptor binding as measured by carbon-11-raclopride (11C-raclopride) has shown to reflect disease severity of Huntington's disease, a genetic disease characterized by selective degeneration of cerebral D2 receptors.[4]

Other studies have investigated the relationship of D2 receptor binding capacity and personality disorders. One study found decreased binding in the detachment personality trait.[5] Radiolabelled raclopride is also commonly used to determine the efficacy and neurotoxicity of dopaminergic drugs.

References

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