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A series of substituted 1 H -indolyl carboxylic acid amides that contain a N -(2-methoxyphenyl)piperazine or N -(2-fluoroethoxy)piperazine group were synthesized and their affinities for human dopamine D 2 , D 3 , and D 4 receptors were determined. Two of these compounds, 14a and 14b , displayed high binding affinity at D 3 ( K  i = 0.18 and 0.4 nM, respectively), and selectivity for D 3  vs. D 2 receptors (87-fold and 60-fold, respectively). These two compounds had low binding affinity at D 4 receptors and σ receptor sites. The intrinsic activity of these compounds at D 2 and D 3 receptors was determined using a forskolin-dependent adenylyl cyclase inhibition assay; both 14a and 14b were found to be partial agonists. Furthermore, for compound 14a , the log D value of 2.85 suggested it has suitable lipophilicity for crossing the blood-brain-barrier.

Synthesis and in vitro pharmacological evaluation of indolyl carboxylic amide analogues as D3 dopamine receptor selective ligands