2000
DOI: 10.1021/jm0009989
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Cyanoindole Derivatives as Highly Selective Dopamine D4Receptor Partial Agonists:  Solid-Phase Synthesis, Binding Assays, and Functional Experiments

Abstract: Traceless linking of diethoxymethyl (DEM)-protected 5- and 6-cyanoindoles and subsequent incorporation of phenylpiperazine derivatives led to the 2- and 3-piperazinylmethyl-substituted cyanoindoles 3a-m. Dopamine receptor binding studies on the final products 3a-m clearly indicated strong and selective recognition of the D(4) subtype which is known as a promising target for the treatment of neuropsychiatric disorders. The most interesting binding properties were observed for the 2-aminomethyl-5-cyanoindoles FA… Show more

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Cited by 66 publications
(48 citation statements)
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“…For an optimized incorporation of [ 131 I]iodide, the precursor concentration should not be less than 7.5 mM (Figure 2 [16][17][18][19] in order to determine receptor affinity and subtype selectivity. Here, we compare K i values determined for the cold compound % 2 to the binding characteristics of FAUC 113 and to those of compound % 1 which were already published.…”
Section: Resultsmentioning
confidence: 99%
“…For an optimized incorporation of [ 131 I]iodide, the precursor concentration should not be less than 7.5 mM (Figure 2 [16][17][18][19] in order to determine receptor affinity and subtype selectivity. Here, we compare K i values determined for the cold compound % 2 to the binding characteristics of FAUC 113 and to those of compound % 1 which were already published.…”
Section: Resultsmentioning
confidence: 99%
“…The mitogenesis experiments were done with a CHO10001A cell line stably transfected with the rat dopamine D 4.2 receptor according to literature [18]. In brief, cells were grown in MEM α-medium supplemented with fetal calf serum, L-glutamine, penicillin G, streptomycin and hygromycin B at 37°C under a humidified atmosphere of 5 % CO 2 Ϫ95 % air at a density of 10,000 cells/well.…”
Section: Mitogenesis Assaymentioning
confidence: 99%
“…Gmeiner et al 28 modified the indole 2-position by treating the polymer-bound 2-chloromethylindoles 57 with arylpiperazines (Scheme 14). The compounds obtained were found as highly selective dopamine D 4 receptor partial agonists.…”
Section: Modifications Leading To Tertiary Aminesmentioning
confidence: 99%