Raclopride (FLA-870)

Description: Raclopride (formerly FLA870) is a novel, potent and selective dopamine D2/D3 receptorantagonist, which binds to D2 and D3 receptors with dissociationconstants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very lowaffinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively. Raclopride's selectivity to the cerebral D2 receptors ischaracterized 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. Itcan be radiolabelled with radioisotopes, e.g. 3H or 11C and used as atracer for in vitro imaging (autoradiography) as well as in vivo imagingpositron emission tomography (PET). Images obtained by cerebral PETscanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment ofthe binding capacity of the cerebral D2 dopamine receptor, which can beuseful for the diagnosis of movement disorders.

References: Trends Pharmacol Sci. 1994 Jul; 15(7):264-70.

Related CAS #: 98185-20-7 (tartrate); 84225-95-6 (free base)