Section 42
Chapter 41,613

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

Fortin, M.; Degryse, M.; Petit, F.; Hunt, P.F.

Neuropharmacology 30(4): 409-412


ISSN/ISBN: 0028-3908
PMID: 1677169
DOI: 10.1016/0028-3908(91)90068-m
Accession: 041612598

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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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