Synthesis and in vitro affinity for dopamine D-2 receptor of N-fluorine-substituted analogs of eticlopride.
With the aim of developing fluorinated benzamides that may be useful as radioligands for positron emission tomography, fluorine analogs of eticlopride, in which the N-ethyl group was replaced by 2-fluoroethyl, 3-fluoropropyl and p-fluorobenzyl groups, were synthesized. These derivatives were tested for their ability to displace [3H]spiperone from its specific dopamine D-2 receptor. Their potencies were decreased when compared with eticlopride, but the two fluoroalkylated analogs were in the same order of magnitude as that of haloperidol.
Fukumura
T
T
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Dohmoto
H
H
Maeda
M
M
Fukuzawa
E
E
Kojima
M
M
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism*; D012457:Salicylamides / Q000494:pharmacology*; D013134:Spiperone / Q000378:metabolism
D011954:Receptors, Dopamine; D012457:Salicylamides; D013134:Spiperone; C045989:eticlopride