Comparison between dopamine transporter affinity and self-administration potency of local anesthetics in rhesus monkeys.
Article Details
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Wilcox KM, Paul IA, Woolverton WL
Comparison between dopamine transporter affinity and self-administration potency of local anesthetics in rhesus monkeys.
Eur J Pharmacol. 1999 Feb 19;367(2-3):175-81.
- PubMed ID
- 10078990 [ View in PubMed]
- Abstract
Local anesthetics bind to dopamine transporters and inhibit dopamine uptake in rodent brain. Additionally, local anesthetics are self-administered in rhesus monkeys. The present study determined binding affinities of cocaine and five local anesthetics at dopamine transporters in rhesus monkey brain, and compared binding affinities to published self-administration potencies in rhesus monkeys. The affinity order at dopamine transporters was cocaine > dimethocaine > tetracaine > procaine > or = chloroprocaine > lidocaine. The correlation between dopamine transporter affinities and self-administration potencies was significant. Binding affinities were also determined at sodium (Na2+) channels in rhesus monkey brain. There was not a significant correlation between Na2+ channel affinities and self-administration potencies Local anesthetics with high dopamine transporter and low Na2+ channel affinities were self-administered, whereas those with either high or low affinity at both sites were not consistently self-administered. These data suggest that affinity at dopamine transporters is related to the reinforcing effects of local anesthetics in rhesus monkeys, and Na2+ channel effects may interfere with the reinforcing effect of these drugs.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Chloroprocaine Sodium-dependent dopamine transporter Protein Humans UnknownInhibitorDetails