Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.

  title={Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.},
  author={Smita Patel and Stephen D Freedman and Kerry L Chapman and Frances Emms and Astrid Elizabeth Fletcher and Margaret Knowles and Rose Marwood and G Mcallister and Jeffrey Myers and Nigel Curtis and Janusz J. Kulagowski and Paul D. Leeson and Mark P Ridgill and Melissa Graham and Sannali Matheson and Daniel Rathbone and Alan P. Watt and Linda J. Bristow and Nadia M. J. Rupniak and E. S. Baskin and James J. Lynch and Colman Ragan},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={283 2},
L-745,870,(3-([4-(4-chlorophenyl)piperazin-1-yl]methyl)-1H- pyrollo[2,3-b] pyridine, was identified as a selective dopamine D4 receptor antagonist with excellent oral bioavailability and brain penetration. L-745,870 displaced specific binding of 0.2 nM [3H] spiperone to cloned human dopamine D4 receptors with a binding affinity (Ki) of 0. 43 nM which was 5- and 20-fold higher than that of the standard antipsychotics haloperidol and clozapine, respectively. L-745,870 exhibited high selectivity… CONTINUE READING
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Lack of effect of the dopamine D4 receptor antagonist, L-745,870 on amphetamine-induced behaviours in rodents

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Adverse effects of antipsychotic agents . Do newer agents offer advantages ?

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Adverse effects of antipsychotic agents. Do newer agents offer advantages? Drugs

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L-745,870 (3-{[4-(4-chlorophenyl) piperazin-1-yl] methyl} -1H-pyrollo [2,3-b] pyridine: A high affinity and selective dopamine D4 receptor antagonist

  • S. PATEL, R. M. MARWOOD, +4 authors S. B. FREEDMAN
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  • 1996
3 Excerpts

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