Binding characteristics of remoxipride and its metabolites to dopamine D2 and D3 receptors.
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Mohell N, Sallemark M, Rosqvist S, Malmberg A, Hogberg T, Jackson DM
Binding characteristics of remoxipride and its metabolites to dopamine D2 and D3 receptors.
Eur J Pharmacol. 1993 Jul 6;238(1):121-5. doi: 10.1016/0014-2999(93)90515-j.
- PubMed ID
- 8405075 [ View in PubMed]
- Abstract
The substituted benzamide, remoxipride, is a new atypical antipsychotic agent with good clinical efficacy and low extrapyramidal side-effect potential. In the present study, the in vitro receptor binding properties of remoxipride and several of its metabolites to rat striatal dopamine D2 and cloned human dopamine D2A and D3 receptors were investigated. Remoxipride bound to [3H]raclopride-labelled dopamine D2 receptors in rat striatum with an affinity (Ki) of 113 nM. The significantly lower affinities of remoxipride reported when [3H]spiperone was used as a radioligand are suggested to be due to methodological problems associated with the use of very high-affinity radioligands. Some of the phenolic metabolites of remoxipride found mainly in rat exhibited considerably higher affinities to dopamine D2 and D3 receptors than remoxipride itself. The pyrrolidone metabolites found mainly in the human had very low dopamine D2 and D3 affinities. The present in vitro results suggest that the behavioural effects of remoxipride in rats may reflect the effect of remoxipride and some of its high-affinity metabolites.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Remoxipride Dopamine D2 receptor Protein Humans YesAntagonistDetails Remoxipride Dopamine D3 receptor Protein Humans UnknownAntagonistDetails - Drug Reactions
Reaction Details Details Details
