Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics

  title={Selective inhibition of monoamine neurotransmitter transporters by synthetic local anesthetics},
  author={T. Sato and Shigeo Kitayama and Chieko Mitsuhata and T Ikeda and Katsuya Morita and Toshihiro Dohi},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  • T. Sato, S. Kitayama, T. Dohi
  • Published 17 January 2000
  • Biology, Chemistry
  • Naunyn-Schmiedeberg's Archives of Pharmacology
Abstract. Synthetic local anesthetics (LAs) have been found to have cocaine-like characteristics with some psychotomimetic action, possibly through monoaminergic neurotransmission. To gain insight into the relation between LA action and monoamine transporters, we investigated the effect of synthetic LAs on neurotransmitter transporters, including monoamine transporters. We used cloned transporter cDNAs and examined transient functional expression in COS cells and stable expression in HeLa cells… 
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MAGE-D1 Regulates Expression of Depression-Like Behavior through Serotonin Transporter Ubiquitylation
A novel role for MAGE-D1 in depressive behaviors: modulating SERT ubiquitylation to the serotonin transporter (SERT) is suggested.


In vitro and in vivo effects of cocaine and selected local anesthetics on the dopamine transporter.
Effects of antidepressants on monoamine transporters
Dissection of Dopamine and Cocaine Binding Sites on the Rat Dopamine Transporter Expressed in COS Cells a
Dopamine transporter (DAT) terminates dopaminergic neurotransmission by Na’ and C1dependent reaccumulation of released dopamine (DA) in presynaptic neurons. Cocaine and related drugs bind to these
Cocaine inhibits GABA release in the VTA through endogenous 5-HT
  • D. Cameron, J. Williams
  • Biology, Psychology
    The Journal of neuroscience : the official journal of the Society for Neuroscience
  • 1994
Using intracellular recordings from midbrain dopamine neurons in a brain slice preparation, it is concluded that cocaine acts to modulate the GABA input to A10 dopamine neurons via inhibition of the 5- HT transporter, increasing the concentration of 5-HT at presynaptic5-HT1D receptors.
Serotonin-facilitated dopamine release in vivo: pharmacological characterization.
The receptor specificity of serotonin (5-HT) agonist-induced facilitation of dopamine (DA) release was assessed by using in vivo microdialysis and coperfusion of antagonists with agonists indicated involvement of 5-HT1 and 5- HT3 receptors and a lack of involvement of 6-methyl-5H-thiazolo-1-pyrimidin-5-one receptors.
Cocaine discrimination: relationship to local anesthetics and monoamine uptake inhibitors in C57BL/6 mice
The importance of the dopamine transporter in mediating the discriminative stimulus effects of cocaine in C57 mice is emphasized and the lack of cross generalization between cocaine and procaine suggests that the anesthetic properties of cocaine contribute little toward its discrimination by this mouse strain.
Dopamine transporter site-directed mutations differentially alter substrate transport and cocaine binding.
Results demonstrate that aspartate and serine residues lying within the first and seventh hydrophobic putative transmembrane regions are crucial for DAT function and provide identification of residues differentially important for cocaine binding and for dopamine uptake.
Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter
The molecular identification and pharmacological characterization of the extraneuronal catecholamine transporter is reported, which is unrelated to the family of sodium-driven neuronal monoamine transporters.
Cocaine receptors labeled by [3H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane.
The results show that [ 3H]CFT and [3H]cocaine bind to a similar spectrum of sites in monkey caudate putamen, with a high positive correlation (r, 0.99, p less than 0.001) between the affinities of drugs at sites labeled by [3h]C FT and [4-fluorophenyl)-tropane.