Description
Raclopride is a selective dopamine D
2/D
3 receptor antagonist with K
i values of 1.8, 3.5, 2,400, and 18,000 nM for D
2, D
3, D
4, and D
1 receptors, respectively. It passes the blood brain barrier and can be used in
in vivo binding and autoradiography studies of the dopamine system under normal and pathological conditions such as Huntington’s disease.
Chemical Properties
Yellowish solid
Uses
Raclopride is a potent D2DR/D3DR antagonist.
Uses
neuroleptic;selective dopamine D1/D2 receptors antagonist
Uses
A labelled dopamine receptor
Definition
ChEBI: 3,5-dichloro-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2-hydroxy-6-methoxybenzamide is a member of salicylamides.
Biological Activity
Selective and potent dopamine D 2 /D 3 receptor antagonist (K i values are 1.8, 3.5, 2400 and 18000 nM for D 2 , D 3 , D 4 and D 1 receptors respectively). Centrally active following systemic administration in vivo .
References
[1] M S LIDOW. Dopamine D2 receptors in the cerebral cortex: distribution and pharmacological characterization with [3H]raclopride.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1989, 86 16: 6412-6416. DOI:
10.1073/pnas.86.16.6412[2] GINOVART N. Imaging the dopamine system with in vivo [11C]raclopride displacement studies: understanding the true mechanism.[J]. Molecular Imaging and Biology, 2005, 7 1: 45-52. DOI:
10.1007/s11307-005-0932-0
