Raclopride, a new selective ligand for the dopamine-D2 receptors.
1. The use of raclopride, a new compound of the salicylamide series, as a ligand for the labelling of dopamine-D2 receptors in vitro and in vivo is described. 2. 3H-Raclopride has a high affinity for the dopamine-D2 receptors (Kd = 1 nM in rat striatum) with much less affinity for any other receptor. 3. 3H-Raclopride enters the brain easily and has therefore also been used in in vivo binding and autoradiography. The nonspecific binding is very low both in vitro and in vivo. 4. Raclopride has been labelled with 11C, and is used as a marker for dopamine-D2 receptors in the living human brain using positron emission tomography.
Hall
H
H
Research and Development Laboratories, Astra Alab AB, Södertälje, Sweden.
Köhler
C
C
Gawell
L
L
Farde
L
L
Sedvall
G
G
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D020891:Raclopride; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2; D012457:Salicylamides / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D012457:Salicylamides; D020891:Raclopride