2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist

@article{Nakane20052434Dimethylphenylpiperazin1ylmethy,
  title={2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist},
  author={Masaki Nakane and Marlon D. Cowart and Gin C. Hsieh and Loan N. Miller and Marie E. Uchic and Renjie Chang and Marc A Terranova and D L Donnelly-roberts and Marian T. Namovic and Thomas R. Miller and Jill M. Wetter and Kennan Marsh and Andrew O. Stewart and Jorge D. Brioni and Robert B. Moreland},
  journal={Neuropharmacology},
  year={2005},
  volume={49},
  pages={112-121}
}
2-[4-(3,4-Dimethylphenlyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393) was identified as a potent dopamine D4 receptor antagonist with excellent receptor selectivity. [3H]-spiperone competition binding assays showed that A-381393 potently bound to membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when… Expand
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