Dopamine reuptake inhibitor

Short description: Class of drug

"DARI" redirects here. For other uses, see Dari (disambiguation).

Dopamine reuptake inhibitor

Drug class
Class identifiers
Use| Major depressive disorder, attention-deficit hyperactivity disorder, narcolepsy
Biological target| Dopamine transporter

A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission.[1]

DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been linked to increased susceptibility to addictive behavior given increase in dopaminergic neurotransmission. The dopaminergic pathways are considered to be strong reward centers.[citation not found] Many DRIs such as cocaine are drugs of abuse due to the rewarding effects evoked by elevated synaptic concentrations of dopamine in the brain.

## Contents

* 1 Medical uses
* 2 Pharmacology
* 3 History
* 4 List of DRIs
* 4.1 Selective dopamine reuptake inhibitors
* 4.2 DRIs with substantial activity at other sites
* 4.3 Other DRIs
* 5 See also
* 6 References

## Medical uses

The following drugs have DRI action and have been or are used clinically specifically for this property: amineptine, dexmethylphenidate, difemetorex, 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).[2][3] 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. [4][5]

The wakefulness-promoting agent modafinil and its analogues (e.g., adrafinil, armodafinil) have been approved to treat narcolepsy and shift work sleep disorder.[6] These act as weak (micromolar) DRIs,[7] but this effect does not correlate with wakefulness-promoting effects, suggesting the effect is too weak to be of clinical significance. The conclusion is that these drugs promote wakefulness via some other mechanism.[8][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.[9]

Monoamine reuptake inhibitors, including DRIs, have proven quite effective in managing excessive food consumption and regulating appetite in 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.[10]

## Pharmacology

DRIs may be divisible into two different types with different effects: (1) typical or conventional DRIs like cocaine, WIN-35428 (β-CFT), and methylphenidate that produce potent psychostimulant, euphoric, and reinforcing effects; and (2) atypical DRIs like vanoxerine (GBR-12909), modafinil, benztropine, and bupropion, which do not produce such effects or have greatly reduced such effects.[11] Moreover, atypical DRIs are often dysphoric at high doses.[11]

Typical DRIs may actually be acting as dopamine releasing agent (DRA)-like agents that have been referred to as dopamine transporter (DAT) "inverse agonists" rather than as simple competitive reuptake inhibitors (which is what atypical DRIs are proposed to be).[11] Typical DRIs are similar to substrate-type DRAs in their effects on brain dopamine levels and in their subjective and behavioral effects.[11]

In terms of maximal brain dopamine elevations, typical DRIs or DAT "inverse agonists" can increase levels by 500 to 1,500%, substrate-type DRAs by more than 1,000% (as high as 5,000% or more), and atypical DRIs or competitive reuptake inhibitors by less than or equal to 500%.[11][12]

## History

Until the 1950s, dopamine was thought to only contribute to the biosynthesis of norepinephrine and 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.[13]

## List of DRIs

Only DRIs which are selective for the DAT over the other monoamine transporters (MATs) are listed below. For a list of DRIs that act at multiple MATs, see other monoamine reuptake inhibitor pages such as NDRI and SNDRI.[disputed - discuss]

### Selective dopamine reuptake inhibitors

Neurotransmitter transporter inhibitors

Dopamine transporter inhibitors

* α-Pyrrolidinoisohexanophenone (α-PiHP) - very strong and very selective for the dopamine transporter, with little to no effect on the norepinephrine and serotonin transporters
* 4-Hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone
* Altropane (O-587)
* Amfonelic acid (WIN 25978)
* Amineptine (has a reasonable degree of selectivity for dopamine over norepinephrine reuptake inhibition)
* BTCP (GK-13)
* 3C-PEP
* DBL-583
* Difluoropine (O-620)
* GBR-12783
* GBR-12935
* GBR-13069
* GBR-13098
* GYKI-52895
* Iometopane (β-CIT, RTI-55)
* Ethylphenidate (more selective for DA vs NE reuptake inhibition compared to methylphenidate, but still has a marked effect on both)
* Modafinil (relatively weak but very selective for the dopamine transporter, with little to no effect on the norepinephrine or serotonin transporters)
* Armodafinil (R-enantiomer of modafinil; somewhat more potent at inhibiting DAT than racemic modafinil, with equally negligible action on NET and SERT)
* RTI-229
* Vanoxerine (GBR-12909)

### DRIs with substantial activity at other sites

* Amantadine (also a weak NMDA receptor antagonist)
* Benztropine (also a muscarinic antagonist)
* Bupropion (also a more potent NRI and likely NRA due to bupropion's major metabolite hydroxybupropion)
* Cocaine
* Fluorenol (extremely weak)
* Medifoxamine (relatively weak)
* Metaphit (irreversible; depletes dopamine)
* Methylphenidate (has a mild degree of selectivity for dopamine over norepinephrine reuptake inhibition, although it significantly affects both)
* Dexmethylphenidate (the dextro diastereomer (R,R steriomer) of methylphenidate; is theorized to be more potent (twice as potent on a milli-to-milli basis) than racemic methylphenidate[14])
* Nomifensine (also a norepinephrine reuptake inhibitor; is used for the treatment of clinical depression, attention deficit hyperactivity disorder (ADHD), narcolepsy, and Parkinson's disease).
* Phenylpiracetam
* Isopropylphenidate[15]
* Rimcazole
* Venlafaxine (weak)
* Solriamfetol (also a norepinephrine reuptake inhibitor)

### Other DRIs

* Chaenomeles speciosa (Flowering quince)[16]
* Oroxylin A (found in Oroxylum indicum and Scutellaria baicalensis (Skullcap))[17]

## See also

* Monoamine reuptake inhibitor
* Dopamine agonist

## References

1. ↑ Song, R.; Zhang, H.-Y.; Li, X.; Bi, G.-H.; Gardner, E. L.; Xi, Z.-X. (2012). "Increased vulnerability to cocaine in mice lacking dopamine D3 receptors". Proceedings of the National Academy of Sciences 109 (43): 17675–17680. doi:10.1073/pnas.1205297109. ISSN 0027-8424. PMID 23045656. Bibcode: 2012PNAS..10917675S.
2. ↑ Singh Satendra (2010). "ChemInform Abstract: Chemistry, Design, and Structure-Activity Relationship of Cocaine Antagonists". ChemInform 31 (20): no. doi:10.1002/chin.200020238. https://www.erowid.org/archive/rhodium/pdf/cocaineanalogs.pdf#4. . Page 928 (4th of article) 1st paragraph. Lines 8—11. Mirror hotlink.
3. ↑ "Thermodynamic analyses of the binding of substrates and uptake inhibitors on the neuronal carrier of dopamine labeled with [3H]GBR 12783 or [3H]mazindol". J. Pharmacol. Exp. Ther. 253 (3): 1206–14. 1990. doi:10.1016/S0022-3565(25)13223-0. PMID 2141637.
4. ↑ "Mephedrone and methylenedioxypyrovalerone (MDPV), major constituents of "bath salts," produce opposite effects at the human dopamine transporter". Psychopharmacology 227 (3): 493–9. 2013. doi:10.1007/s00213-013-2967-2. PMID 23371489.
5. ↑ "Actions of cocaine on rat dopaminergic neurones in vitro". Br. J. Pharmacol. 99 (4): 731–5. April 1990. doi:10.1111/j.1476-5381.1990.tb12998.x. PMID 2361170.
6. ↑ "The prevalence and cost of unapproved uses of top-selling orphan drugs". PLOS ONE 7 (2). 2012. doi:10.1371/journal.pone.0031894. PMID 22363762. Bibcode: 2012PLoSO...731894K.
7. ↑ Loland, C.J.; M. Mereu; O.M. Okunola; J. Cao; T.E. Prisinzano; T. Kopajtic; L. Shi; J.L. Katz et al. (1 September 2012). "R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse.". Biol. Psychiatry 72 (5): 405–13. doi:10.1016/j.biopsych.2012.03.022. PMID 22537794.
8. ↑ "Neurobiology of addiction". Curr. Opin. Neurobiol. 6 (2): 243–51. 1996. doi:10.1016/S0959-4388(96)80079-1. PMID 8725967.
9. ↑ "Development of the dopamine transporter selective RTI-336 as a pharmacotherapy for cocaine abuse". AAPS J 8 (1): E196–203. 2006. doi:10.1208/aapsj080124. PMID 16584128.
10. ↑ Kintscher, U (2012). "Reuptake Inhibitors of Dopamine, Noradrenaline, and Serotonin". Appetite Control. Handbook of Experimental Pharmacology. 209. pp. 339–347. doi:10.1007/978-3-642-24716-3_15. ISBN 978-3-642-24715-6.
11. ↑ 11.0 11.1 11.2 11.3 11.4 Heal, David J.; Gosden, Jane; Smith, Sharon L. (2014-12-01). "Dopamine reuptake transporter (DAT) "inverse agonism" – A novel hypothesis to explain the enigmatic pharmacology of cocaine". Neuropharmacology. CNS Stimulants 87: 19–40. doi:10.1016/j.neuropharm.2014.06.012. ISSN 0028-3908. PMID 24953830. https://www.sciencedirect.com/science/article/abs/pii/S0028390814002342.
12. ↑ "Amphetamine, past and present--a pharmacological and clinical perspective". J Psychopharmacol 27 (6): 479–496. June 2013. doi:10.1177/0269881113482532. PMID 23539642.
13. ↑ Jack R. Cooper; Floyd E. Bloom; Robert H. Roth (1996). "9". The Biochemical Basis of Neuropharmacology (7th ed.). Oxford University Press, Inc. p. 293.
14. ↑ Markowitz, JS; Patrick, KS (June 2008). "Differential pharmacokinetics and pharmacodynamics of methylphenidate enantiomers: does chirality matter?". Journal of Clinical Psychopharmacology 28 (3 Suppl 2): S54-61. doi:10.1097/JCP.0b013e3181733560. PMID 18480678. https://journals.lww.com/psychopharmacology/abstract/2008/06002/differential_pharmacokinetics_and_pharmacodynamics.4.aspx. Retrieved 28 May 2024.
15. ↑ Markowitz, John S.; Zhu, Hao-Jie; Patrick, Kennerly S. (2013-12-18). "Isopropylphenidate: An Ester Homolog of Methylphenidate with Sustained and Selective Dopaminergic Activity and Reduced Drug Interaction Liability" (in en). Journal of Child and Adolescent Psychopharmacology 23 (10): 648–654. doi:10.1089/cap.2013.0074. ISSN 1044-5463. PMID 24261661.
16. ↑ "Dopamine transporter inhibitory and antiparkinsonian effect of common flowering quince extract". Pharmacology Biochemistry and Behavior 90 (3): 363–71. September 2008. doi:10.1016/j.pbb.2008.03.014. PMID 18485464.
17. ↑ Yoon, Seo Young; dela Peña, Ike; Kim, Sung Mok; Woo, Tae Sun; Shin, Chan Young; Son, Kun Ho; Park, Haeil; Lee, Yong Soo et al. (2013). "Oroxylin A improves attention deficit hyperactivity disorder-like behaviors in the spontaneously hypertensive rat and inhibits reuptake of dopamine in vitro". Archives of Pharmacal Research 36 (1): 134–140. doi:10.1007/s12272-013-0009-6. ISSN 0253-6269. PMID 23371806.

* v
* t
* e

Stimulants

Adamantanes|

* Adapromine
* Amantadine
* Bromantane
* Memantine
* Rimantadine

Adenosine antagonists|

* 8-Chlorotheophylline
* 8-Cyclopentyltheophylline
* 8-Phenyltheophylline
* Aminophylline
* Caffeine
* CGS-15943
* Dimethazan
* Paraxanthine
* SCH-58261
* Theobromine
* Theophylline

Alkylamines|

* Cyclopentamine
* Cypenamine
* Cyprodenate
* Heptaminol
* Isometheptene
* Levopropylhexedrine
* Methylhexaneamine
* Octodrine
* Propylhexedrine
* Tuaminoheptane

Ampakines|

* CX-516
* CX-546
* CX-614
* CX-691
* CX-717
* IDRA-21
* LY-404,187
* LY-503,430
* Nooglutyl
* Org 26576
* PEPA
* S-18986
* Sunifiram
* Unifiram

Arylcyclohexylamines|

* Benocyclidine
* Dieticyclidine
* Esketamine
* Eticyclidine
* Gacyclidine
* Ketamine
* Phencyclamine
* Phencyclidine
* Rolicyclidine
* Tenocyclidine
* Tiletamine

Benzazepines|

* 6-Br-APB
* SKF-77434
* SKF-81297
* SKF-82958

Cholinergics|

* A-84,543
* A-366,833
* ABT-202
* ABT-418
* AR-R17779
* Altinicline
* Anabasine
* Arecoline
* Bradanicline
* Cotinine
* Cytisine
* Dianicline
* Epibatidine
* Epiboxidine
* GTS-21
* Ispronicline
* Nicotine
* PHA-543,613
* PNU-120,596
* PNU-282,987
* Pozanicline
* Rivanicline
* Sazetidine A
* SIB-1553A
* SSR-180,711
* TC-1698
* TC-1827
* TC-2216
* Tebanicline
* UB-165
* Varenicline
* WAY-317,538

Convulsants|

* Anatoxin-a
* Bicuculline
* DMCM
* Flurothyl
* Gabazine
* Haldol
* Pentetrazol
* Picrotoxin
* Strychnine
* Thujone

Eugeroics|

* Adrafinil
* Armodafinil
* CRL-40,940
* CRL-40,941
* Fluorenol
* Modafinil

Oxazolines|

* 4-Methylaminorex
* Aminorex
* Clominorex
* Cyclazodone
* Fenozolone
* Fluminorex
* Pemoline
* Thozalinone

Phenethylamines|

* 1-(4-Methylphenyl)-2-aminobutane
* 1-Methylamino-1-(3,4-methylenedioxyphenyl)propane
* 2-Fuoroamphetamine
* 2-Fuoromethamphetamine
* 2-OH-PEA
* 2-Phenyl-3-aminobutane
* 2,3-MDA
* 3-Fuoroamphetamine
* 3-Fluoroethamphetamine
* 3-Fluoromethcathinone
* 3-Methoxyamphetamine
* 3-Methylamphetamine
* 3,4-DMMC
* 4-BMC
* 4-CMC
* 4-Fluoroamphetamine
* 4-Fluoromethamphetamine
* 4-MA
* 4-Methylbuphedrone
* 4-Methylcathinone
* 4-MEAP
* 4-MMA
* 4-Methylpentedrone
* 4-MTA
* 6-FNE
* AL-1095
* Alfetamine
* a-Ethylphenethylamine
* Amfecloral
* Amfepentorex
* Amfepramone
* Amidephrine
* 2-Amino-1,2-dihydronaphthalene
* 2-Aminoindane
* 5-(2-Aminopropyl)indole
* 2-Aminotetralin
* Acridorex
* Amphetamine (Dextroamphetamine, Levoamphetamine)
* Amphetaminil
* Arbutamine
* β-Methylphenethylamine
* β-Phenylmethamphetamine
* Benfluorex
* Benzedrone
* Benzphetamine
* BDB
* BOH
* 3-Benzhydrylmorpholine
* BPAP
* Buphedrone
* Bupropion
* Butylone
* Camfetamine
* Cathine
* Cathinone
* Chlorphentermine
* Cilobamine
* Cinnamedrine
* Clenbuterol
* Clobenzorex
* Cloforex
* Clortermine
* Cypenamine
* D-Deprenyl
* Denopamine
* Dimethoxyamphetamine
* Dimethylamphetamine
* Dimethylcathinone
* Dobutamine
* DOPA (Dextrodopa, Levodopa)
* Dopamine
* Dopexamine
* Droxidopa
* EBDB
* Ephedrine
* Epinephrine
* Epinine
* Etafedrine
* Ethcathinone
* Ethylnorepinephrine
* Ethylone
* Etilamfetamine
* Etilefrine
* Famprofazone
* Fencamfamin
* Fencamine
* Fenethylline
* Fenfluramine (Dexfenfluramine, Levofenfluramine)
* Fenproporex
* Feprosidnine
* Flephedrone
* Fludorex
* Formetorex
* Furfenorex
* Gepefrine
* Hexapradol
* Hexedrone
* HMMA
* Hordenine
* 4-Hydroxyamphetamine
* 5-Iodo-2-aminoindane
* Ibopamine
* Indanylamphetamine
* Iofetamine
* Isoetarine
* Isoethcathinone
* Isoprenaline
* L-Deprenyl (Selegiline)
* Lefetamine
* Lisdexamfetamine
* Lophophine
* MBDB
* MDA (tenamfetamine)
* MDBU
* MDEA
* MDMA (midomafetamine)
* MDMPEA
* MDOH
* MDPR
* MDPEA
* Mefenorex
* Mephedrone
* Mephentermine
* Metanephrine
* Metaraminol
* Mesocarb
* Methamphetamine (Dextromethamphetamine, Levomethamphetamine)
* Methoxamine
* Methoxyphenamine
* MMA
* Methcathinone
* Methedrone
* Methoxyphenamine
* Methylenedioxycathinone
* Methylone
* Mexedrone
* MMDA
* MMDMA
* MMMA
* Morforex
* N,alpha-Diethylphenylethylamine
* N-Ethylbuphedrone
* N-Ethylhexedrone
* N,N-Dimethylphenethylamine
* Naphthylamphetamine
* Nisoxetine
* Norepinephrine
* Norfenefrine
* Norfenfluramine
* Normetanephrine
* L-Norpseudoephedrine
* Octopamine (drug)
* Orciprenaline
* Ortetamine
* Oxifentorex
* Oxilofrine
* PBA
* PCA
* PCMA
* PHA
* Pentorex
* Pentedrone
* Pentylone
* Phenatine
* Phenpromethamine
* Phentermine
* Phenylalanine
* Phenylephrine
* Phenylpropanolamine
* Pholedrine
* PIA
* PMA
* PMEA
* PMMA
* PPAP
* Phthalimidopropiophenone
* Prenylamine
* Propylamphetamine
* Pseudoephedrine
* Ropinirole
* Salbutamol (Levosalbutamol)
* Sibutramine
* Solriamfetol
* Synephrine
* Theodrenaline
* Tiflorex
* Tranylcypromine
* Tyramine
* Tyrosine
* Xylopropamine
* Zylofuramine

Phenylmorpholines|

* 3-Fluorophenmetrazine
* Fenbutrazate
* Fenmetramide
* G-130
* Manifaxine
* Morazone
* Morforex
* Oxaflozane
* PD-128,907
* Phendimetrazine
* Phenmetrazine
* 2-Phenyl-3,6-dimethylmorpholine
* Pseudophenmetrazine
* Radafaxine

Piperazines|

* 2C-B-BZP
* 3C-PEP
* BZP
* CM156
* DBL-583
* GBR-12783
* GBR-12935
* GBR-13069
* GBR-13098
* GBR-13119
* MeOPP
* MBZP
* oMPP
* Vanoxerine

Piperidines|

* 1-Benzyl-4-(2-(diphenylmethoxy)ethyl)piperidine
* 2-Benzylpiperidine
* 2-Methyl-3-phenylpiperidine
* 3,4-Dichloromethylphenidate
* 4-Benzylpiperidine
* 4-Fluoromethylphenidate
* 4-Methylmethylphenidate
* Desoxypipradrol
* Difemetorex
* Diphenylpyraline
* Ethylnaphthidate
* Ethylphenidate
* Methylnaphthidate
* Isopropylphenidate
* JZ-IV-10
* Methylphenidate (Dexmethylphenidate)
* Nocaine
* Phacetoperane
* Pipradrol
* Propylphenidate
* SCH-5472

Pyrrolidines|

* 2-Diphenylmethylpyrrolidine
* 5-DBFPV
* α-PPP
* α-PBP
* α-PHP
* α-PHPP
* α-PVP
* α-PVT
* Diphenylprolinol
* DMPVP
* FPOP
* FPVP
* MDPPP
* MDPBP
* MPBP
* MPHP
* MPPP
* MOPVP
* MOPPP
* Indapyrophenidone
* MDPV
* Naphyrone
* PEP
* Picilorex
* Prolintane
* Pyrovalerone

Racetams|

* Oxiracetam
* Phenylpiracetam
* Phenylpiracetam hydrazide

Tropanes|

* 4-fluorotropacocaine
* 4'-Fluorococaine
* Altropane (IACFT)
* Brasofensine
* CFT (WIN 35,428)
* β-CIT (RTI-55)
* Cocaethylene
* Cocaine
* Dichloropane (RTI-111)
* Difluoropine
* FE-β-CPPIT
* FP-β-CPPIT
* Ioflupane (123I)
* Norcocaine
* PIT
* PTT
* RTI-31
* RTI-32
* RTI-51
* RTI-112
* RTI-113
* RTI-120
* RTI-121 (IPCIT)
* RTI-126
* RTI-150
* RTI-177
* RTI-229
* RTI-336
* RTI-354
* RTI-371
* RTI-386
* Salicylmethylecgonine
* Tesofensine
* Troparil (β-CPT, WIN 35,065-2)
* Tropoxane
* WF-23
* WF-33

Tryptamines|

* 4-HO-αMT
* 4-Methyl-αET
* 4-Methyl-αMT
* 5-Chloro-αMT
* 5-Fluoro-αMT
* 5-MeO-αET
* 5-MeO-αMT
* 5-MeO-DIPT
* 6-Fluoro-αMT
* 7-Methyl-αET
* αET
* αMT

Others|

* 2-MDP
* 3,3-Diphenylcyclobutanamine
* Amfonelic acid
* Amineptine
* Amiphenazole
* Atipamezole
* Atomoxetine
* Bemegride
* Benzydamine
* BTQ
* BTS 74,398
* Centanafadine
* Ciclazindol
* Clofenciclan
* Cropropamide
* Crotetamide
* D-161
* Desipramine
* Diclofensine
* Dimethocaine
* Efaroxan
* Etamivan
* Fenisorex
* Fenpentadiol
* Gamfexine
* Gilutensin
* GSK1360707F
* GYKI-52895
* Hexacyclonate
* Idazoxan
* Indanorex
* Indatraline
* JNJ-7925476
* Lazabemide
* Leptacline
* Lomevactone
* LR-5182
* Mazindol
* Meclofenoxate
* Medifoxamine
* Mefexamide
* Methamnetamine
* Methastyridone
* Methiopropamine
* Naphthylaminopropane
* Nefopam
* Nikethamide
* Nomifensine
* O-2172
* Oxaprotiline
* PNU-99,194
* PRC200-SS
* Rasagiline
* Rauwolscine
* Rubidium chloride
* Setazindol
* Tametraline
* Tandamine
* Thiopropamine
* Thiothinone
* Trazium
* UH-232
* Yohimbine

ATC code: N06B

* v
* t
* e

ADHD pharmacotherapies

CNS stimulants|

* Amphetamine (Mixed amphetamine salts, Levoamphetamine, Dextroamphetamine, Lisdexamfetamine)
* Methamphetamine
* Methylphenidate
* Dexmethylphenidate

Non-classical
CNS stimulants|

* Atomoxetine
* Modafinil

α2-adrenoceptor
agonists|

* Clonidine
* Guanfacine

Antidepressants|

* Amitriptyline
* Bupropion
* Buspirone
* Desipramine
* Duloxetine
* Imipramine
* Milnacipran
* Moclobemide
* Nortriptyline
* Reboxetine
* Venlafaxine

Miscellaneous/others|

* Amantadine
* Carbamazepine

Related articles|

* Attention deficit hyperactivity disorder (ADHD)
* Attention deficit hyperactivity disorder management
* Monoamine releasing agent
* Dopamine (DA)
* Dopamine transporter (DAT)
* Dopamine reuptake inhibitor (DRI)
* Norepinephrine (NE)
* Norepinephrine transporter (NET)
* Norepinephrine reuptake inhibitor (NRI)
* Serotonin (5-HT)
* Serotonin transporter (SERT)
* Selective serotonin reuptake inhibitor (SSRI)
* Serotonin-norepinephrine reuptake inhibitor (SNRI)
* Norepinephrine-dopamine reuptake inhibitor (NDRI)
* Serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI)

Template:Wakefulness-promoting agents

* v
* t
* e

Antiobesity agents/Anorectics (A08)

Central|

| Stimulants|

* 4-Methylamphetamine‡
* Amfecloral
* Amfepentorex
* Amfepramone
* Aminorex‡
* Amphetamine
* Amphetaminil
* Atomoxetine
* Benfluorex‡
* Benzphetamine
* Bupropion (+naltrexone; +zonisamide†)
* Cathine
* Cathinone
* Chlorphentermine
* Ciclazindol
* Clobenzorex
* Cloforex
* Clominorex
* Clortermine
* Dexfenfluramine‡
* Dextroamphetamine
* Dexmethylphenidate
* Difemetorex‡
* Dimethylcathinone
* Ephedrine
* Ephedra‡
* Etilamfetamine
* Etolorex
* Fenbutrazate
* Fencamfamin
* Fenethylline
* Fenfluramine‡ (+phentermine‡)
* Fenproporex
* Fludorex
* Fluminorex
* Furfenorex‡
* Indanorex
* Khat
* Levopropylhexedrine
* Lisdexamfetamine
* Manifaxine
* Mazindol
* Mefenorex
* Methamphetamine
* Methylphenidate
* Norfenfluramine
* Pemoline
* Pentorex
* Phendimetrazine
* Phenethylamine
* Phenmetrazine
* Phentermine (+topiramate)
* Phenylpropanolamine
* Picilorex
* Pipradrol
* Prolintane
* Propylhexedrine
* Pseudoephedrine
* Pyrovalerone
* Radafaxine
* Reboxetine
* Setazindol
* Sibutramine‡
* Synephrine
* Tesofensine
* Viloxazine
* Xylopropamine
* Zylofuramine

|

Cannabinoid
receptor antagonists|

* Drinabant§
* Ibipinabant§
* Otenabant§
* Rimonabant‡
* Rosonabant§
* Surinabant§
* Taranabant§

Others|

* 5-HTP
* Beloranib§
* Galactomannan
* Guar gum
* Glucomannan
* L-DOPA
* L-Phenylalanine
* L-Tryptophan
* L-Tyrosine
* Lorcaserin
* Lu AA-33810
* Metformin
* Naltrexone
* Naloxone
* Oxyntomodulin
* P57
* Peptide YY
* Topiramate
* Velneperit§
* Yohimbine (Yohimbe)
* Zonisamide
* Water

Peripheral|

* Cetilistat
* 2,4-Dinitrophenol‡
* Dirlotapide
* Mitratapide
* Oleoyl-estrone
* Orlistat
* Simmondsin
* Sterculia

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

* v
* t
* e

Euphoriants

* μ-Opioid receptor agonists (opioids) (e.g., morphine]], heroin, hydrocodone, oxycodone, opium, kratom)
* α2δ subunit-containing voltage-dependent calcium channels blockers (gabapentinoids) (e.g., gabapentin, pregabalin, phenibut)
* AMPA receptor antagonists (e.g., perampanel)
* CB1 receptor agonists (cannabinoids) (e.g., THC]], cannabis)
* Dopamine receptor agonists (e.g., levodopa)
* Dopamine releasing agents (e.g., amphetamine, methamphetamine]], MDMA, Chemistry:Mephedrone

See also: Recreational drug use

* v
* t
* e

Monoamine reuptake inhibitors

DAT
(DRIs)|

* Piperazines: DBL-583
* GBR-12783
* GBR-12935
* GBR-13069
* GBR-13098
* Nefazodone
* Vanoxerine

* Piperidines: 4-Fluoropethidine
* Benocyclidine (BTCP)
* Desoxypipradrol
* Dexmethylphenidate
* Difemetorex
* Ethylphenidate
* HDMP-28
* Methylphenidate
* Pethidine (meperidine)
* Phencyclidine
* Pipradrol
* Tenocyclidine

* Pyrrolidines: Diphenylprolinol
* MDPV
* Naphyrone
* Prolintane
* Pyrovalerone

* Tropanes: Altropane
* Benzatropine (benztropine)
* Brasofensine
* CFT
* Cocaine
* Dichloropane
* Difluoropine
* Etybenzatropine (ethybenztropine)
* FE-β-CPPIT
* FP-β-CPPIT
* Ioflupane (123I)
* RTI-55
* RTI-112
* RTI-113
* RTI-121
* RTI-126
* RTI-150
* RTI-177
* RTI-229
* RTI-336
* Tesofensine
* Troparil
* Tropoxane
* WF-11
* WF-23
* WF-31
* WF-33

* Others: Adrafinil
* Amifitadine
* Armodafinil
* Amfonelic acid
* Amineptine
* Ansofaxine
* BTQ
* BTS 74,398
* Bupropion
* Chaenomeles speciosa
* Ciclazindol
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine
* Diclofensine
* Didesmethylsibutramine
* Dimethocaine
* Diphenylpyraline
* Dizocilpine (MK-801)
* DOV-102,677
* DOV-216,303
* Efavirenz
* Ephenidine
* Esketamine
* EXP-561
* Fencamfamin
* Fezolamine
* Fluorenol
* GYKI-52895
* Indatraline
* Ketamine
* Lefetamine
* Levophacetoperane
* Liafensine
* LR-5182
* Manifaxine
* Mazindol
* Medifoxamine
* Mesocarb
* Metaphit
* MIN-117 (WF-516)
* Modafinil
* Nefopam
* Nomifensine
* NS-2359
* O-2172
* Oroxylin A
* Perafensine
* Pridefine
* Radafaxine
* Rimcazole
* Sertraline
* Sibutramine
* Solriamfetol
* Tametraline
* Tedatioxetine
* Tripelennamine
* Venlafaxine

NET
(NRIs)|

* Selective norepinephrine reuptake inhibitors: Amedalin
* Alseroxylon
* Ciclazindol
* Daledalin
* Edivoxetine
* Esreboxetine
* Lortalamine
* Mazindol
* Nisoxetine
* Reboxetine
* Talopram
* Talsupram
* Tandamine
* Teniloxazine
* Viloxazine

* Norepinephrine–dopamine reuptake inhibitors: Amineptine
* Bupropion
* Fencamine
* Fencamfamin
* Hydroxybupropion
* Lefetamine
* Levophacetoperane
* LR-5182
* Manifaxine
* Methylphenidate
* Nomifensine
* O-2172
* Radafaxine
* Solriamfetol

* Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
* BTS-54505
* CP-39,332
* Desvenlafaxine
* Duloxetine
* Eclanamine
* Levomilnacipran
* McN-5652
* Milnacipran
* N-Methyl-PPPA
* Nafenodone
* PPPA
* Tofenacin
* Venlafaxine
* WY-45233

* Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
* Amifitadine
* Ansofaxine
* Bicifadine
* Brasofensine
* Centanafadine
* Cocaine
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine
* Diclofensine
* Didesmethylsibutramine
* DOV-102677
* DOV-216303
* EXP-561
* Fezolamine
* HDMP-28
* Indatraline
* JNJ-7925476
* JZ-IV-10
* Liafensine
* Mazindol
* Naphyrone
* Nefazodone
* Nefopam
* NS-2359
* Perafensine
* PRC200
* Pridefine
* SEP-228431
* SEP-228432
* Sibutramine
* Tedatioxetine
* Tesofensine
* Tropanes (e.g., cocaine)

* Tricyclic antidepressants: Amitriptyline
* Butriptyline
* Cianopramine
* Clomipramine
* Desipramine
* Dosulepin (dothiepin)
* Doxepin
* Imipramine
* Lofepramine
* Melitracen
* Nortriptyline
* Protriptyline
* Trimipramine

* Tetracyclic antidepressants: Amoxapine
* Maprotiline
* Mianserin
* Oxaprotiline
* Setiptiline

* Others: Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine)
* Antipsychotics (e.g., loxapine, ziprasidone)
* Arylcyclohexylamines (e.g., ketamine, phencyclidine)
* Dopexamine
* Ephenidine
* Ginkgo biloba
* Indeloxazine
* Nefazodone
* Opioids (e.g., Desmetramadol|Desmetramadol]]]], methadone, pethidine (meperidine), tapentadol, tramadol, Levorphanol

SERT
(SRIs)|

* Selective serotonin reuptake inhibitors: Alaproclate
* Centpropazine
* Cericlamine
* Citalopram
* Dapoxetine
* Desmethylcitalopram
* Didesmethylcitalopram
* Escitalopram
* Femoxetine
* Fluoxetine
* Fluvoxamine
* Indalpine
* Ifoxetine
* Norfluoxetine
* Omiloxetine
* Panuramine
* Paroxetine
* PIM-35
* Pirandamine
* RTI-353
* Seproxetine
* Sertraline
* Zimelidine

* Selective serotonin reuptake inhibitors and serotonin receptor modulators: Etoperidone
* Litoxetine
* Lubazodone
* LY-393558
* SB-649915
* TGBA01AD
* Trazodone
* Vilazodone
* Vortioxetine

* Serotonin–norepinephrine reuptake inhibitors: Atomoxetine (tomoxetine)
* Bicifadine
* BTS-54505
* CP-39332
* Desvenlafaxine
* Duloxetine
* Eclanamine
* Levomilnacipran
* McN-5652
* Milnacipran
* N-Methyl-PPPA
* PPPA
* Tofenacin
* Venlafaxine
* WY-45233

* Serotonin–norepinephrine–dopamine reuptake inhibitors: 3,3-Diphenylcyclobutanamine
* Amifitadine
* Ansofaxine
* Bicifadine
* Brasofensine
* Centanafadine
* Cocaine
* Dasotraline
* Desmethylsertraline
* Desmethylsibutramine
* Diclofensine
* Didesmethylsibutramine
* DOV-102677
* DOV-216303
* EXP-561
* Fezolamine
* HDMP-28
* Indatraline
* JNJ-7925476
* JZ-IV-10
* Liafensine
* Mazindol
* Naphyrone
* Nefazodone
* Nefopam
* NS-2359
* Perafensine
* PRC200
* Pridefine
* SEP-228431
* SEP-228432
* Sibutramine
* Tedatioxetine
* Tesofensine
* Tropanes (e.g., cocaine)

* Tricyclic antidepressants: Amitriptyline
* Cianopramine
* Clomipramine
* Cyanodothiepin
* Desipramine
* Dosulepin (dothiepin)
* Doxepin
* Imipramine
* Lofepramine
* Nortriptyline
* Pipofezine
* Protriptyline

* Others: A-80426
* Amoxapine
* Antihistamines (e.g., brompheniramine, [[Chemistry:Chlorphenchlorphenamine]], dimenhydrinate, diphenhydramine, mepyramine (pyrilamine), pheniramine, Chemistry:Tripelennamine

VMATs|

* Amiodarone
* Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
* APP
* AZIK
* Bietaserpine
* Deserpidine
* Deutetrabenazine
* Dihydrotetrabenazine
* Efavirenz
* GBR-12935
* GZ-793A
* Ibogaine
* Ketanserin
* Lobeline
* Methoxytetrabenazine
* Reserpine
* Rose bengal
* Tetrabenazine
* Valbenazine
* Vanoxerine (GBR-12909)

Others|

* DAT enhancers: Luteolin

* DAT modulators: Agonist-like: SoRI-9804
* SoRI-20040; Antagonist-like: SoRI-20041

See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins

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Original source: https://en.wikipedia.org/wiki/Dopamine reuptake inhibitor. Read more

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*[v]: View this template
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*[ADHD]: Attention-deficit hyperactivity disorder
*[CNS]: central nervous system
*[DAT]: Dopamine transporter
*[DRIs]: Dopamine reuptake inhibitors
*[NET]: Norepinephrine transporter
*[NRIs]: Norepinephrine reuptake inhibitors
*[SERT]: Serotonin transporter
*[SRIs]: Serotonin reuptake inhibitors
*[VMATs]: Vesicular monoamine transporters