77Br-p-bromospiperone: a ligand for in vivo labelling of dopamine receptors.
A high striatum: cerebellum ratio of 77Br-p-bromospiperone (77Br-BrSp) was observed in rat brain following tail vein injection of the drug. Striatal 77Br-BrSp was stereospecifically displaced by the isomers of flupenthixol. After chronic haloperidol administration striatal dopamine receptor supersensitivity was demonstrated both by increased 3H-spiperone binding to striatal membranes in vitro and by increased striatal 77Br-BrSp content. These results confirm and extend previous findings and enhance interest in the use of 77Br-BrSp for the in vivo assessment of central dopamine receptors in man.
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D001966:Bromine; D002090:Butyrophenones / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D005475:Flupenthixol / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D008297:Male; D011868:Radioisotopes; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism*; D013134:Spiperone / Q000031:analogs & derivatives / Q000378:metabolism*; D014018:Tissue Distribution
D002090:Butyrophenones; D011868:Radioisotopes; D011954:Receptors, Dopamine; D013134:Spiperone; C026326:4-bromospiperone; D005475:Flupenthixol; D006220:Haloperidol; D001966:Bromine