Dopamine reuptake inhibitor

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Dopamine reuptake inhibitors
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"DARI" redirects here. For other uses, see Dari (disambiguation).
Dopamine reuptake inhibitor
attention-deficit hyperactivity disorder, narcolepsy
Biological targetDopamine transporter
Legal status
In Wikidata

A dopamine reuptake inhibitor (DRI) is a class of

extracellular concentrations of dopamine and increase in dopaminergic neurotransmission.[1]

DRIs are used in the treatment of

drugs of abuse due to the rewarding effects evoked by elevated synaptic concentrations of dopamine in the brain
.

Society and culture

History of use

Until the 1950s, dopamine was thought to only contribute to the

epinephrine. It was not until dopamine was found in the brain in similar levels as norepinephrine that the possibility was considered that its biological role might be other than the synthesis of the catecholamines.[2]

Pharmacotherapeutic uses

The following drugs have DRI action and have been or are used clinically specifically for this property:

fencamfamine, lefetamine, levophacetoperane, medifoxamine, mesocarb, methylphenidate, nomifensine, pipradrol, prolintane, and pyrovalerone
.

The following drugs are or have been used clinically and possess only weak DRI action, which may or may not be clinically-relevant: adrafinil, armodafinil, bupropion, mazindol, modafinil, nefazodone, sertraline, and sibutramine.

The following drugs are or have been clinically used but only coincidentally have DRI properties: benzatropine, diphenylpyraline, etybenzatropine, ketamine, nefopam, pethidine (meperidine), and tripelennamine.

The following are a selection of some particularly notably abused DRIs: cocaine, ketamine, MDPV, naphyrone, and phencyclidine (PCP). Amphetamines, including amphetamine, methamphetamine, MDMA, cathinone, methcathinone, mephedrone, and methylone, are all DRIs as well, but are distinct in that they also behave, potentially more potently, as dopamine releasing agents (DRAs) (due to Yerkes–Dodson's law, 'more potently stimulated' may not equal more optimally functionally stimulated). There are very distinct differences in the mode of action between dopamine releasers/substrates & dopamine re-uptake inhibitors; the former are functionally entropy-driven (i.e., relating to hydrophobicity) and the latter are enthalpy-driven (i.e., relating conformational change).[3][4] Reuptake inhibitors such as cocaine induce hyperpolarization of cloned human DAT upon oocytes that are naturally found on neurons, whereas releasing agents induce de-polarization of the neuron membrane.[dubious – discuss][5][6]

The

disputed – discuss
]

DRIs have been explored as potential

antiaddictive agents in the context of replacement therapy strategies, analogous to nicotine replacement for treating tobacco addiction and methadone replacement in the case of opioid addiction. DRIs have been explored as treatment for cocaine addiction, and have shown to alleviate cravings and self-administration.[10]

Monoamine reuptake inhibitors, including DRIs, have shown effectiveness as therapy for excessive food intake and appetite control for obese patients. Though such pharmacotherapy is still available, the majority of stimulant anorectics marketed for this purpose have been withdrawn or discontinued due to adverse side effects such as hypertension, valvulopathy, and drug dependence.[11]

List of DRIs

Only DRIs which are selective for the DAT over the other

disputed – discuss
]

Selective dopamine reuptake inhibitors

Neurotransmitter transporter inhibitors
  Dopamine transporter inhibitors

DRIs with substantial activity at other sites

Other DRIs

See also

References

  1. PMID 23045656
    .
  2. ^ Jack R. Cooper; Floyd E. Bloom; Robert H. Roth (1996). "9". The Biochemical Basis of Neuropharmacology (7th ed.). Oxford University Press, Inc. p. 293.
  3. doi:10.1002/chin.200020238.. Page 928 (4th of article) 1st paragraph. Lines 8—11. Mirror hotlink.
  4. PMID 2141637
    .
  5. PMID 23371489
    .
  6. PMID 2361170
    .
  7. PMID 22363762
    .
  8. PMID 22537794
    .
  9. S2CID 25378856
    .
  10. PMID 16584128
    .
  11. PMID 22249822
    .
  12. ^ "Isopropylphenidate: An Ester Homolog of Methylphenidate with Sustained and Selective Dopaminergic Activity and Reduced Drug Interaction Liability". Archived from the original on 3 June 2021.
  13. S2CID 40114711
    .
  14. S2CID 23927252
    .

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