3-Aminomethylbiphenyls. A New Class of Dopamine Receptor Ligands
A series of 3-aminomethylbiphenyls were prepared in three steps from 3-phenylbenzoic acid and their affinities for the D2, D3 and D4 dopamine receptor subtypes determined. Most of the compounds described contained unique amine subunits of known dopaminergic agents. The compounds containing the amino tails present in the antipsychotic drugs haloperidol, pimozide and miliperidine displayed selectivity for the D2 receptor. Five-fold selectivity for the D4 receptor was observed in the compound 1-(3-biphenyl)-4-(2-pyrimidyl)piperazine. This selectivity for D4 vs. D2 receptors is comparable to that observed with the atypical antipsychotic clozapine.
Thurkauf, Andrew,Yuan, Jun,Chen, Xi,Wasley, Jan W. F.,Paneitz, Gregory,Meade, Robin,Woodruff, Kristine Harris,Huston, Kevin,Ross, Philip C.
A series of some novel N-(1-ethyl-2-pyrrolidinylmethyl)benzamides was synthesized and tested for dopamine receptor blockade in vivo by the ability to block the apomorphine syndrome in the rat.Several compounds were considerably more potent than sulpiride as dopamine receptor blockers and displayed low liability to induce extrapyramidal side effects (catalepsy) in the rat.The blockade of dopamine receptor activity in vivo was mainly confined to the levorotatory isomers having the S absolute configuration.The structure-activity relationships are discussed.
Florvall, Lennart,Oegren, Sven-Ove
p. 1280 - 1286
(2007/10/02)
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