Relative affinities of dopaminergic drugs at dopamine D2 and D3 receptors.
Quantitative autoradiography was used to evaluate the pharmacological profile of dopamine D2-like receptors labeled by [125I]iodosulpiride. Caudate/putamen, a brain region associated primarily with dopamine D2 receptor mRNA, was used as a prototypical D2 tissue; cerebellar lobule X (D3 mRNA associated), as a D3 tissue. 7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4- tetrahydronaphthalene) exhibited selectively for cerebellar receptors (24-fold), followed by quinpirole (6-fold). Haloperidol and domperidone were 4- and 18-fold more potent at striatal receptors, respectively. These data are in close agreement with that derived from dopamine D2 and D3 receptor-expressing cell lines.
Levant
B
B
DuPont Merck Pharmaceutical Company, Wilmington, DE 19880, USA.
Grigoriadis
D E
DE
De Souza
E B
EB
D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive; D001921:Brain / Q000648:ultrastructure*; D016466:CHO Cells / Q000648:ultrastructure; D002421:Caudate Nucleus / Q000648:ultrastructure; D002531:Cerebellum / Q000648:ultrastructure; D006224:Cricetinae; D015259:Dopamine Agents / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008297:Male; D011699:Putamen / Q000648:ultrastructure; D051381:Rats; D017207:Rats, Sprague-Dawley; D011954:Receptors, Dopamine / Q000378:metabolism*; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3; D012680:Sensitivity and Specificity; D013469:Sulpiride / Q000031:analogs & derivatives / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism
D015259:Dopamine Agents; C493595:Drd3 protein, rat; D007457:Iodine Radioisotopes; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D013764:Tetrahydronaphthalenes; C045105:iodosulpride; D013469:Sulpiride; C031349:7-hydroxy-2-N,N-dipropylaminotetralin