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general/norepinephrine-dopamine-reuptake-inhibitors

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Norepinephrine–dopamine reuptake inhibitor

Drug that inhibits the reuptake of norepinephrine and dopamine


Summary

Drug that inhibits the reuptake of norepinephrine and dopamine

FieldValue
Name
ImageMethylphenidate-2D-skeletal.svg
ImageClassskin-invert-image
Width250px
CaptionMethylphenidate, one of the most widely used NDRIs.
UseADHD, depression, narcolepsy
Mechanism_of_actionreuptake inhibitor
Biological_targetnorepinephrine transporter (NET),
dopamine transporter (DAT)
Drugs.com

dopamine transporter (DAT) | Drugs.com = A norepinephrine–dopamine reuptake inhibitor (NDRI) is a type of drug that inhibits the reuptake of the monoamine neurotransmitters norepinephrine and dopamine and thereby increases extracellular levels of these neurotransmitters and noradrenergic and dopaminergic neurotransmission. They work by competitively and/or noncompetitively inhibiting the norepinephrine transporter (NET) and dopamine transporter (DAT).

NDRIs are used clinically in the treatment of conditions including attention deficit hyperactivity disorder (ADHD), narcolepsy, and depression. Examples of well-known NDRIs include methylphenidate and bupropion.

A closely related type of drug is a norepinephrine–dopamine releasing agent (NDRA).

List of NDRIs

Many NDRIs exist, including the following:

  • Amineptine (Survector, Maneon, Directim)
  • Bupropion (Wellbutrin, Zyban)
  • Desoxypipradrol (2-DPMP)
  • Dexmethylphenidate (Focalin)
  • Difemetorex (Cleofil)
  • Diphenylprolinol (D2PM)
  • Ethylphenidate
  • Fencamfamine (Glucoenergan, Reactivan)
  • Fencamine (Altimina, Sicoclor)
  • Lefetamine (Santenol)
  • Methylenedioxypyrovalerone (MDPV)
  • Methylphenidate (Ritalin, Concerta, Metadate, Methylin, Foquest)
  • Nomifensine (Merital)
  • O-2172
  • Phenylpiracetam (Phenotropil, Carphedon)
  • Pipradrol (Meretran)
  • Prolintane (Promotil, Katovit)
  • Pyrovalerone (Centroton, Thymergix)
  • Solriamfetol (Sunosi)
  • Tametraline (CP-24,411)
  • WY-46824}}

Some NDRIs, such as methylphenidate, may not act as simple NDRIs but rather as DAT "inverse agonists" (and possibly also analogously at the NET as well). If this theory is correct, then methylphenidate and other agents like cocaine may not be acting primarily as monoamine reuptake inhibitors but instead as robust monoamine releasing agent-esque drugs, albeit via a different mechanism of action than conventional substrate-type monoamine releasing agents.

Norepinephrine–dopamine releasing agents (NDRAs) like amphetamine and methamphetamine not only induce monoamine release but also act as monoamine reuptake inhibitors to a lesser extent and hence are additionally NDRIs.

References

References

  1. Stephen M. Stahl. (2 March 2009). "Antidepressants". Cambridge University Press.
  2. (2004). "A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor.". Primary Care Companion to the Journal of Clinical Psychiatry.
  3. (December 2014). "Dopamine reuptake transporter (DAT) "inverse agonism"--a novel hypothesis to explain the enigmatic pharmacology of cocaine". Neuropharmacology.
  4. (October 2003). "Monoamine transporters and psychostimulant drugs". Eur J Pharmacol.
  5. (January 2001). "Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin". Synapse.
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