Raclopride

Raclopride

Clinical data
ATC code	none
Pharmacokinetic data
Biological half-life	20 min
Identifiers
IUPAC name 3,5-dichloro-N-[[(2S)-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide
CAS Number	84225-95-6 N
PubChem CID	3033769
IUPHAR/BPS	94
ChemSpider	2298373 Y
UNII	430K3SOZ7G
ChEMBL	CHEMBL8809 Y
Chemical and physical data
Formula	C15H20Cl2N2O3
Molar mass	347.236 g/mol
3D model (Jmol)	Interactive image
SMILES Clc1c(O)c(c(OC)c(Cl)c1)C(=O)NC[C@H]2N(CC)CCC2
InChI 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 Y Key:WAOQONBSWFLFPE-VIFPVBQESA-N Y
NY (what is this?)

Raclopride is a synthetic compound that acts as a selective antagonist on D₂dopamine receptors.

Its selectivity to the cerebral D₂ receptors is characterized by its respective K_i-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D₂, D₃, D₄ and D₁ receptors respectively.

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 genetical disease characterized by selective degeneration of cerebral D₂ receptors.

Other studies have investigated the relationship of D₂ receptor binding capacity and personality disorders. For example, one study found decreasing binding with the personality trait detachment. Radiolabelled raclopride is also commonly used to determine the efficacy and neurotoxicity of dopaminergic drugs.