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.
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
T
T
Fukumura
H
H
Dohmoto
M
M
Maeda
E
E
Fukuzawa
M
M
Kojima
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