Potential dopamine receptor ligand

Le Foil B, Schwartz J-C, Sokoloff P (2000) Dopamine D3 receptor agents as potential new medications for drag addiction. Fur Psychiatry 15 140-146 Le Foil B, Schwartz J-C, Sokoloff P (2003a) Disruption of nicotine conditioning by dopamine D3 receptor ligands. Mol Psychiatry 8 225-230... 

Another inventive extension of click chemistry is the concept of cUck-resins that promote solid phase supported reactions to work under nearly perfect conditions, fulfilling the requirements of click chemistry [32, 33]. This approach has enabled the assembly of a library of carboxylic arene bioisoesters, with the general formula V [34] as potential dopamine D4 receptor ligands [35]. In essence, the authors completed parallel synthesis of bioactive tert-amines V, utilizing triazolyl-methylacrylate 7 as a linker. The product was readily generated from the commercial azidomethyl substituted polystyrene 5 and propargyl acrylate 6 via Cu(I) catalyzed 1,3-dipolar cycloaddition (Scheme 15.4). 

A series of 5- and 6-substituted isoquinuclidine 4-amino-5-chloromethoxy benzoates and benzamides (11-16) was found to have binding affinity for 5-HT3, 5-HT4 and dopamine (DA) D2 receptors. In general, although 5-substituted ISQs demonstrated more potential as 5-HT3 ligands while also possessing 5-HT4 and D2 properties, the 6-substituted derivatives afforded the most promising compounds in terms of both receptor affinity and selectivity [20],... 

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