Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine

@article{Tol1991CloningOT,
  title={Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine},
  author={Hubert H.M. Van Tol and James R. Bunzow and H C Guan and Roger K. Sunahara and Philip Seeman and Hyman B. Niznik and Olivier Civelli},
  journal={Nature},
  year={1991},
  volume={350},
  pages={610-614}
}
DOPAMINE receptors belong to the family of G protein-coupled receptors. On the basis of the homology between these receptors, three different dopamine receptors (D1,D2,D3) have been cloned1–7. Dopamine receptors are primary targets for drugs used in the treatment of psychomotor disorders such as Parkinson's disease and schizophrenia8,9. In the management of socially withdrawn and treatment-resistant schizophrenics, clozapine10 is one of the most favoured antipsychotics because it does not cause… Expand
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  • Medicine
  • Pharmacology & therapeutics
  • 2001
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Because of distinct aspects of regulation of the D3 receptor, it represents a unique target for therapeutic intervention in schizophrenia without high potential for unintended side effects such as tardive dyskinesia. Expand
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TLDR
The results suggest the D3 receptor as an important target for antipsychotic drug action, and D2/D3 receptor selective antagonists as promising therapeutic agents. Expand
Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor.
TLDR
It is demonstrated that pipamperone, an antipsychotic, acts as a pharmacological chaperone and by doing so, increases the expression level of the dopamine D4 receptor. Expand
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TLDR
The results with the antipsychotic agents tested, support the concept that dopamine D4 receptor selectivity may confer clozapine-like antipsychotics efficacy and furthermore that dopamineD2 receptor selectiveness may confer side effect liability (extrapyramidal side effects and tardive dyskinesia). Expand
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This receptor has been characterized on the basis of three criteria: the deduced amino-acid sequence which reveals that it is a member of the family of G-protein-coupled receptors; the tissue distribution of the mRNA which parallels that of the D2 dopamine receptor; and the pharmacological profile of mouse fibroblast cells transfected with the cDNA. Expand
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