Ketamine stereoselectively inhibits rat dopamine transporter

@article{Nishimura1999KetamineSI,
  title={Ketamine stereoselectively inhibits rat dopamine transporter},
  author={Mitsuhiro Nishimura and K. Sato},
  journal={Neuroscience Letters},
  year={1999},
  volume={274},
  pages={131-134}
}
Effects of Ketamine and Ketamine Metabolites on Evoked Striatal Dopamine Release, Dopamine Receptors, and Monoamine Transporters
  • A. Can, P. Zanos, T. Gould
  • Biology, Psychology
    The Journal of Pharmacology and Experimental Therapeutics
  • 2016
TLDR
Neither ketamine’s enantiomers nor its metabolites had affinity for DA receptors or the DA, noradrenaline, and serotonin transporters (up to 10 μM), suggesting that neither the side effects nor antidepressant actions of ketamine or ketamine metabolites are associated with direct effects on mesolimbic DAergic neurotransmission.
The ketamine analogue methoxetamine generalizes to ketamine discriminative stimulus in rats
TLDR
The present findings suggest that investigation of ‘ketamine-like compounds’ should explore not only substances with chemical analogy and common molecular mechanisms with ketamine, but also with similar psychopharmacological effects.
(R)-Ketamine Induces a Greater Increase in Prefrontal 5-HT Release Than (S)-Ketamine and Ketamine Metabolites via an AMPA Receptor-Independent Mechanism
TLDR
R-Ketamine strongly activates the prefrontal serotonergic system through an AMPA receptor-independent mechanism and provides a neurochemical basis for the underlying pharmacological differences between ketamine enantiomers and their metabolites.
The Prodrug 4-Chlorokynurenine Causes Ketamine-Like Antidepressant Effects, but Not Side Effects, by NMDA/GlycineB-Site Inhibition
TLDR
4-Cl-KYN administration was not associated with the rewarding and psychotomimetic effects of ketamine, and did not induce locomotor sensitization or stereotypic behaviors, providing further support for antagonism of the glycineB site for the rapid treatment of treatment-resistant depression without the negative side effects seen with ketamine or other channel-blocking NMDA receptor antagonists.
Up-regulation of noradrenaline transporter in response to prolonged exposure to ketamine
TLDR
It is demonstrated that prolonged exposure to ketamine increases the functional activity of NAT and its mRNA, which may imply that ketamine negatively modulates sympathetic nervous activity through an up-regulation of NAT during long anaesthesia.
NMDA receptor antagonists ketamine and PCP have direct effects on the dopamine D2 and serotonin 5-HT2 receptors—implications for models of schizophrenia
TLDR
Ketamine and PCP may not produce a selective hypoglutamate state, but more likely produce a non-selective multi-system neurochemical perturbation via direct and indirect effects.
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Ketamine Inhibits Monoamine Transporters Expressed in Human Embryonic Kidney 293 Cells
TLDR
The result suggests that the ketamine‐induced inhibition of monoamine transporters might contribute to its psychotomimetic and sympathomimetic effects through potentiating monoaminergic neurotransmission.
Synergistic Inhibition of Muscarinic Signaling by Ketamine Stereoisomers and the Preservative Benzethonium Chloride
TLDR
Because S(+) ketamine is a significantly more potent analgesic, it should have less muscarinic inhibitory action than R(‐) ketamine when used in clinically equivalent doses, and if reconstituted with a different preservative, Ketalar might be a less potent mus carinic antagonist.
Effects of ketamine on sensory perception: evidence for a role of N-methyl-D-aspartate receptors.
TLDR
In healthy volunteers, the most obvious effect of subanesthetic doses of both enantiomers was altered sensory perception, and (S)-Ketamine was 4 times as potent as (R)-ketamine in reducing pain perception and in causing auditory and visual disturbances.
Comparative pharmacology of the ketamine isomers. Studies in volunteers.
TLDR
It is concluded that the more potent S(+) isomer of ketamine was associated with a more rapid recovery of psychomotor skills than the currently used racemic mixture.
Cloning and expression of a functional serotonin transporter from rat brain
TLDR
A large family of related gene products expressed in rodent brain is identified from two highly conserved regions of the transporters for noradrenaline and γ-aminobutyric acid, and one of these products hybridizes to a single 3.7-kilobase RNA restricted to rat midbrain and brainstem, where it is highly enriched within the serotonergic raphe complex.
Expression cloning of a cocaine-and antidepressant-sensitive human noradrenaline transporter
TLDR
A complementary DNA clone encoding a human noradrenaline transporter is isolated and the predicted protein sequence demonstrates significant amino-acid identity with the Na+/γ-aminobutyric acid transporter, thus identifying a new gene family for neurotransmitter transporter proteins.
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