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Comparison between dopamine transporter affinity and self-administration potency of local anesthetics in rhesus monkeys.

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.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Wilcox KM,Paul IA,Woolverton WL

doi

10.1016/s0014-2999(98)00967-4

keywords:

subject

Has Abstract

pub_date

1999-02-19 00:00:00

pages

175-81

issue

2-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(98)00967-4

journal_volume

367

pub_type

杂志文章

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