Amphetamine‐type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin

@article{Rothman2001AmphetaminetypeCN,
  title={Amphetamine‐type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin},
  author={Richard B. Rothman and Michael H. Baumann and Christina M. Dersch and D V Romero and Kenner C. Rice and F. Ivy Carroll and John S. Partilla},
  journal={Synapse},
  year={2001},
  volume={39}
}
A large body of evidence supports the hypothesis that mesolimbic dopamine (DA) mediates, in animal models, the reinforcing effects of central nervous system stimulants such as cocaine and amphetamine. The role DA plays in mediating amphetamine‐type subjective effects of stimulants in humans remains to be established. Both amphetamine and cocaine increase norepinephrine (NE) via stimulation of release and inhibition of reuptake, respectively. If increases in NE mediate amphetamine‐type… 

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References

SHOWING 1-10 OF 63 REFERENCES

Neurochemical neutralization of methamphetamine with high‐affinity nonselective inhibitors of biogenic amine transporters: a pharmacological strategy for treating stimulant abuse

An in vitro assay is established which selectively detects transporter substrates and used to profile the ability of a lead compound, indatraline, to block the releasing effects of METH and MDMA at the DA, 5‐HT, and NE transporters.

Dopamine ligands and the stimulus effects of amphetamine: animal models versus human laboratory data

Data regarding the effects of dopamine agonists and antagonists on the discriminative stimulus effects of amphetamine in animals and its subjective effects in humans are reviewed.

Subjective responses to d-amphetamine alone and after pimozide pretreatment in normal, healthy volunteers

High Dose Pimozide Does Not Block Amphetamine-Induced Euphoria in Normal Volunteers

  • L. BrauerH. Wit
  • Psychology, Biology
    Pharmacology Biochemistry and Behavior
  • 1997

The interaction of cocaine with serotonin dorsal raphe neurons. Single-unit extracellular recording studies.

  • K. CunninghamJ. Lakoski
  • Biology, Chemistry
    Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
  • 1990
The hypothesis that the inhibitory effects of cocaine on 5- HT DRN neurons are mediated by increased 5-HT available for interaction with5-HT1A impulse-regulating autoreceptors in the DRN is supported, as a consequence of cocaine-induced blockade of 5-ht reuptake processes.

Physiologic, subjective, and behavioral effects of amphetamine, methamphetamine, ephedrine, phenmetrazine, and methylphenidate in man

This study suggests that it is unlikely that these central actions in man are a consequence of the release of norepinephrine in the brain, and suggests that these five agents share a common mode of central action.

Doses of GBR12909 that suppress cocaine self‐administration in non‐human primates substantially occupy dopamine transporters as measured by [11C] WIN35,428 PET scans

These data strongly suggest that occupancy for the DA transporter by GBR explains its ability to attenuate cocaine‐induced increases in extracellular DA and to suppress cocaine self‐administration and suggest that experimental human studies of orally administered GBR to test the DA hypothesis of cocaine addiction should use doses that produce at least 70% occupancy of theDA transporter.

Discriminative stimulus effects of d-amphetamine, methylphenidate and diazepam in humans

...