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

ABSTRACT: A series of substituted 1H-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 D₂, D₃, and D₄ receptors were determined. Two of these compounds, 14a and 14b, displayed high binding affinity at D₃ (K_i = 0.18 and 0.4 nM, respectively), and selectivity for D₃vs. D₂ receptors (87-fold and 60-fold, respectively). These two compounds had low binding affinity at D₄ receptors and σ receptor sites. The intrinsic activity of these compounds at D₂ and D₃ receptors was determined using a forskolin-dependent adenylyl cyclase inhi

SUBMITTER: Tu Z 

PROVIDER: S-EPMC3804115 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature