NGD 94-1 as an agonist at human recombinant dopamine D4.4 receptors expressed in HEK293 cells

  • Eur J Pharmacol. 1999 May 21;372(3):R9-10. doi: 10.1016/s0014-2999(99)00254-x.
L Gazi  1 ,  B Sommer ,  J Nozulak ,  P Schoeffter
Affiliations
  • 1. Nervous System Therapeutic Area, Novartis Pharma Research, Novartis Pharma, Basel, Switzerland.
PMID: 10395031 DOI: 10.1016/s0014-2999(99)00254-x
Abstract

The atypical antipsychotic, clozapine has some selectivity for dopamine D4 receptors and is a silent antagonist at these receptors. NGD 94-1 (2-phenyl-4(5)-[4-(2-pyrimidinyl)-piperazin-1-yl-methyl]-imidazole ) is a highly selective dopamine D4 receptor ligand recently introduced as a putative antipsychotic mimicking the dopamine D4 receptor antagonist effects of clozapine. We show that NGD 94-1 is not silent. It behaved as an agonist in human embryonic kidney 293 cells expressing human recombinant dopamine D4.4 receptors. This questions the clinical use of NGD 94-1.

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