Literature DB >> 1677169

The dopamine D2 agonists RU 24213 and RU 24926 are also kappa-opioid receptor antagonists.

M Fortin1, M Degryse, F Petit, P F Hunt.   

Abstract

The di-(phenethyl)-amine derivatives, RU 24213 and RU 24926 are widely used as selective dopamine D2-receptor agonists. Binding studies now show that they also have affinity for the kappa-opioid receptor. Their affinity is not greatly reduced in the presence of NaCl/GTP, suggesting an antagonist action. This is confirmed for RU 24926, the more active of the two, using the field-stimulated rabbit vas-deferens. With respect to the mu-receptor, RU 24926 shows low binding affinity and also an antagonist effect. These results demonstrate kappa- as well as mu-antagonist activity in a novel chemical series. Moreover, since the kappa-receptor may regulate dopamine release, the results of experiments using these compounds as dopamine D2 agonists should be interpreted with caution.

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Year:  1991        PMID: 1677169     DOI: 10.1016/0028-3908(91)90068-m

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN: 0028-3908            Impact factor:   5.250


  3 in total

Review 1.  Biased Opioid Ligands.

Authors:  Abdelfattah Faouzi; Balazs R Varga; Susruta Majumdar
Journal:  Molecules       Date:  2020-09-16       Impact factor: 4.411

2.  Structurally Related Kappa Opioid Receptor Agonists with Substantial Differential Signaling Bias: Neuroendocrine and Behavioral Effects in C57BL6 Mice.

Authors:  Amelia D Dunn; Brian Reed; Catherine Guariglia; Alexandra M Dunn; Joshua M Hillman; Mary Jeanne Kreek
Journal:  Int J Neuropsychopharmacol       Date:  2018-09-01       Impact factor: 5.176

Review 3.  Development of Diphenethylamines as Selective Kappa Opioid Receptor Ligands and Their Pharmacological Activities.

Authors:  Helmut Schmidhammer; Filippo Erli; Elena Guerrieri; Mariana Spetea
Journal:  Molecules       Date:  2020-11-02       Impact factor: 4.411

  3 in total

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