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Chu W, Tu Z, McElveen E, Xu J, Taylor M, Luedtke RR, Mach RH: Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
A series of N-(2-methoxyphenyl) piperazine and N-(2,3-dichlorophenyl) piperazine analogs were prepared and their affinities for dopamine D (2), D (3), and D (4) receptors were measured in vitro. Binding studies were also conducted to determine if the compounds bound to sigma (sigma (1) and sigma (2)) and serotonin (5-HT (1A), 5-HT (2A), 5-HT (2B), 5-HT (2C), 5-HT (3), 5-HT (4), 5-HT (5), 5-HT (6), and 5-HT (7)) receptors. The results of the current study revealed a number of compounds (12b, 12c, 12e, and 12g) having a high affinity for D (3) (K (i) at D (3) receptors ranging from 0.3 to 0.9 nM) versus D (2) (K (i) at D (2) receptors ranging from 40 to 53 nM) receptors and a log P value indicating that they should readily cross the blood brain barrier (log P = 2.6-3.5). All of the compounds evaluated in this study had a high affinity for serotonin 5-HT (1A) receptors. These compounds may be useful as probes for studying the behavioral pharmacology of the dopamine D (3) receptor, as well as lead compounds for the development of radiotracers for studying D (3) receptor regulation in vivo with the functional imaging technique, positron emission tomography. |
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