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Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors

  • Original Articles
  • Antiemetic, Dopamine, 5-Hydroxytryptamine Receptors
  • Published:
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Summary

The affinities of 11 drugs for both dopamine D2 and 5-hydroxytryptamine3 (5-HT3) receptor sites were determined in brain membranes. The five “traditional” antiemetics (chlorpromazine, prochlorperazine, droperidol, fluphenazine, and domperidone) displayed high affinity (<20 nM)for dopamine D2 receptors in corpus striatum but were inactive at 5-HT3 receptors. In contrast, five recently developed 5-HT3 antagonists (BRL 43694, ICS 205-930, zacopride, Lilly 278584, and MDL 72222) displayed nanomolar affinity for the 5-HT3 site but were inactive (>10,000 nM) at the dopamine D2 receptor. Metoclopramide was unique among these agents in that it was similarly potent at dopamine D2 (240±60 n M) and 5-HT3 (120±30nM) receptors.

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Authors and Affiliations

  1. Department of Neurology, Stanford University Medical Center, 94305, Stanford, CA, USA

    Anne Hamik & Stephen J. Peroutka

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  1. Anne Hamik
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  2. Stephen J. Peroutka
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Hamik, A., Peroutka, S.J. Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors. Cancer Chemother. Pharmacol. 24, 307–310 (1989). https://doi.org/10.1007/BF00304763

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  • DOI: https://doi.org/10.1007/BF00304763

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