Raclopride

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]

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
ChemSpider
UNII
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
 ☒NcheckY (what is this?)  (verify)

Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-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 genetic disease characterized by selective degeneration of cerebral D2 receptors.[3]

Other studies have investigated the relationship of D2 receptor binding capacity and personality disorders. One study found decreased binding in the detachment personality trait.[4] Radiolabelled raclopride is also commonly used to determine the efficacy and neurotoxicity of dopaminergic drugs.

References
  1. Köhler C, Hall H, Ogren SO, Gawell L (1985). "Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain". Biochemical Pharmacology. 34 (13): 2251–9. doi:10.1016/0006-2952(85)90778-6. PMID 4015674.
  2. Ishibashi K, Ishii K, Oda K, Mizusawa H, Ishiwata K (2010). "Competition between 11C-raclopride and endogenous dopamine in Parkinson's disease". Nucl Med Commun. 31 (2): 159–66. doi:10.1097/MNM.0b013e328333e3cb. PMID 19966595. S2CID 205821715.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  3. Antonini A, Leenders KL, Spiegel R, Meier D, Vontobel P, Weigell-Weber M, Sanchez-Pernaute R, de Yébenez JG, Boesiger P, Weindl A, Maguire RP (1996). "Striatal glucose metabolism and dopamine D2 receptor binding in asymptomatic gene carriers and patients with Huntington's disease". Brain. 119 (6): 2085–95. doi:10.1093/brain/119.6.2085. PMID 9010012.
  4. Farde L, Gustavsson JP, Jönsson E (1997). "D2 dopamine receptors and personality traits". Nature. 385 (6617): 590. Bibcode:1997Natur.385..590F. doi:10.1038/385590a0. PMID 9024656. S2CID 4235650.
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