dopamine reuptake inhibitor

• ドパミン再取り込み阻害薬、ドパミン再取り込み阻害剤

関

dopamine uptake inhibitor

WordNet

1. limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"
2. control and refrain from showing; of emotions, desires, impulses, or behavior (同)bottle up, suppress
3. limit the range or extent of; "Contact between the young was inhibited by strict social customs"
4. a substance that retards or stops an activity
5. a monoamine neurotransmitter found in the brain and essential for the normal functioning of the central nervous system; as a drug (trade names Dopastat and Intropin) it is used to treat shock and hypotension (同)Dopastat, Intropin
6. a process of using up or consuming again; "psychopharmacologists discovered that amine reuptake is a process that inactivates monoamine neurotransmitters" (同)re-uptake

PrepTutorEJDIC

1. 〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》
2. 抑制する人(物) / 化学反応抑制剤

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/10/19 13:52:49」(JST)

wiki en

[Wiki en表示]

A dopamine reuptake inhibitor (DRI) is a type of drug that acts as a reuptake inhibitor for the neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the post-synaptic neuron is blocked from re-entering the pre-synaptic neuron. This, in turn, leads to increased extracellular concentrations of dopamine and therefore an increase in dopaminergic neurotransmission.

DRIs are frequently used in the treatment of conditions like ADHD and narcolepsy on account of their psychostimulant effects and in the treatment of obesity due to their appetite suppressant properties. They have also been used as antidepressants in the treatment of mood disorders, but their use for this indication has been limited on account of their abuse potential and legal restriction. Lack of Dopamine uptake and the increase in extracellular levels of dopamine have been linked to increased susceptibility to addictive behavior due to the increase in dopaminergic neurotransmission. The dopaminergic pathways are considered to be strong reward centers. In addition, many DRIs such as cocaine are drugs of abuse due to the rewarding effects evoked by elevated synaptic concentrations of dopamine in the brain.

Due to their strong rewarding and reinforcing properties, DRIs are notorious for their high abuse potential and liability to cause cravings, addiction, and dependence. DRIs such as cocaine and methylphenidate and combination releasing agents such as amphetamine, methamphetamine, and MDMA ("ecstasy") are widely used recreationally throughout the world.

Society and culture

History of use

Until the 1950s, dopamine was thought to be nothing but part of the synthesis of norepinephrine and epinephrine. It was not until dopamine was found in the brain in same levels as norepinephrine that it was considered that dopamine might have a biological role other than the synthesis of the catecholamines.

Pharmacotherapeutic uses

Norepinephrine-dopamine reuptake inhibition is used as an antidepressant in the form of bupropion, the only norepinephrine-dopamine reuptake inhibitor (NDRI) approved by the Food and Drug Administration. Dopamine supplementation is also utilized as a means to counter act depression. Though no supplement exists that contains dopamine, certain supplements contain nutrients known to aid in dopamine production such as tyrosine, ginkgo biloba, and certain B-vitamins.

Recently the FDA approved wakefulness-promoter and potential anti-apathy medication Modafinil and its derivatives - approved to treat narcolepsy and shift work sleep disorder - were revealed to function through the DRI mechanism. It is used off-label as a method of counteracting the apathy component of depression, Alzheimer's disease, Chagas' disease, Creutzfeldt-Jakob disease, dementia, Korsakoff's syndrome, excessive vitamin D; hypothyroidism and other conditions.

DRIs have been explored as potential pharmacotherapeutics because of their ability to replace rewards received from other drugs. DRIs have been successfully used to serve as nicotine replacements in cases of smoking addictions well as methadone replacements in the case of heroin addiction. DRIs have been explored as potential substitutes for cocaine addiction, and have been shown to alleviate cravings and self-administration.

Monoamine reuptake inhibitors, including DRIs, have also been shown to be effective as therapy for food intake and appetite control for obese subjects. Most marketed drugs for this purpose have been withdrawn due to adverse side-effects such as increase in blood pressure and high abuse potential.

Bupropion

Preclinical and clinical data demonstrate that bupropion acts via dual inhibition of norepinephrine and dopamine reuptake, which constitutes a novel mechanism of antidepressant action. As such, bupropion is associated with a unique clinical profile with efficacy comparable to that of other antidepressants. Devoid of clinically significant serotonergic effects or direct effects on postsynaptic receptors, bupropion—the only currently available NDRI—is as effective as other antidepressants but does not cause common antidepressant-associated side-effects such as sexual dysfunction, weight gain, and sedation. Data supports the use of bupropion as a first-line antidepressant as well as its possible utility as augmentation therapy.

List of DRIs

3D structure of RTI-470, a high-affinity and selective DAT ligand

Many DRIs exist, including the following:

Selective dopamine reuptake inhibitors

• Amineptine (has a reasonable degree of selectivity for dopamine reuptake inhibition over norepinephrine reuptake inhibition)
• Altropane (O-587)
• Amfonelic acid (WIN 25978)

• BTCP (GK-13)

• DBL-583

• Difluoropine (O-620)

• GBR-12935

• GYKI-52895

• Iometopane (β-CIT, RTI-55)

• RTI-229

• Vanoxerine (GBR-12909)

DRIs with activity at other sites

• Medifoxamine (Cledial)

Other DRIs

• Chaenomeles speciosa (Flowering Quince)
• Hyperforin, Adhyperforin (Two of the chief active constituents of St. John's wort act as a reuptake inhibitors of various other neurotransmitters including the other monoamine neurotransmitters, serotonin and norepinephrine, with approximately equal affinity)

Dopamine-controlling drugs

• Bupropion
• Pramipexole

• Cabergoline

Note: Only DRIs selective for the DAT over the other monoamine transporters (MATs) are listed here. For a list of DRIs that act at multiple MATs, see the other monoamine reuptake inhibitor pages such as NDRI and SNDRI.

Additional note: Dopamine releasing agents (DRAs) such as psychostimulants of the amphetamine class also act as DRIs secondarily to their releasing action. To distinguish between DRIs and DRAs, however, the latter are not included in the above list. For a list of DRAs, see the releasing agent article.

See also

• Monoamine reuptake inhibitor

References

UpToDate Contents

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• 1. 非定型抗うつ薬：薬理学、投与方法、および副作用 atypical antidepressants pharmacology administration and side effects
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• 3. ドーパミンの腎臓作用 renal actions of dopamine
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English Journal

• Effects of the triple reuptake inhibitor amitifadine on extracellular levels of monoamines in rat brain regions and on locomotor activity.

• Golembiowska K, Kowalska M, Bymaster FP.SourceDepartment of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, 31-343 Krakow, Poland.
• Synapse (New York, N.Y.).Synapse.2012 May;66(5):435-44. doi: 10.1002/syn.21531. Epub 2012 Feb 15.
• Major depressive disorder is a prevalent disease, and current pharmacotherapy is considered to be inadequate. It has been hypothesized that a triple reuptake inhibitor (TRI) that activates dopamine (DA) neurotransmission in addition to serotonin and norepinephrine (NE) circuitries may result in enha
• PMID 22213370

• Nomifensine alters sex differences in striatal dopaminergic function.

• Poth LS, O'Connell BP, McDermott JL, Dluzen DE.SourceDepartment of Anatomy and Neurobiology, Northeast Ohio Medical University, 4209 State Route 44, PO Box 95, Rootstown, Ohio 44272-0095.
• Synapse (New York, N.Y.).Synapse.2012 Mar 5. doi: 10.1002/syn.21554. [Epub ahead of print]
• A series of three experiments are presented in which the acute effects of the catecholamine reuptake inhibitor, nomifensine, upon striatal dopaminergic function are compared in female and male mice. In Experiment 1, treatment with nomifensine (5 mg/kg), at 30-minutes prior to injection of methamphet
• PMID 22389194

Japanese Journal

• Molecular Docking and Panicolytic Effect of 8-Prenylnaringenin in the Elevated T-Maze

• Chemical and Pharmaceutical Bulletin 62(12), 1231-1237, 2014
• NAID 130004703715

• Effects of Bupropion and Pramipexole on Cell Proliferation in the Hippocampus of Adrenocorticotropic Hormone-Treated Rats

• Biological and Pharmaceutical Bulletin 37(2), 327-330, 2014
• NAID 130003390932

• Milnacipran enhances the control of impulsive action by activating D1-like receptors in the infralimbic cortex

• Psychopharmacology 225(2), 495-504, 2013-01
• NAID 120005358927

Related Links

• Dopamine reuptake inhibitor - Depression Wiki - Wikia

Dopamine Reuptake Inhibitors or Dopamine Uptake Inhibitors are compounds that inhibit the... ... Dopamine Reuptake Inhibitors or Dopamine Uptake Inhibitors are compounds that inhibit the reuptake of the neurotransmitter dopamine after it is released and used at the synapse.

• What Is a Dopamine Reuptake Inhibitor? (with pictures)

In psychopharmacology, a dopamine reuptake inhibitor is a class of drug that is designed to inhibit the action of the dopamine transporter. The dopamine transporter is a protein that helps end the action of dopamine, a ...

Related Pictures

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★リンクテーブル★

リンク元	「dopamine uptake inhibitor」「ドパミン再取り込み阻害剤」「ドパミン再取り込み阻害薬」
関連記事	「inhibit」「inhibitor」

「dopamine uptake inhibitor」

　　[★]

• ドパミン取り込み阻害薬、ドーパミン取り込み阻害薬、ドパミン取り込み阻害剤、ドーパミン取り込み阻害剤、ドパミン取り込み抑制薬、ドーパミン取り込み抑制薬

関

dopamine reuptake inhibitor

「ドパミン再取り込み阻害剤」

　　[★]

英

dopamine reuptake inhibitor

関

ドパミン取り込み阻害薬、ドパミン再取り込み阻害薬、ドーパミン取り込み阻害剤

「ドパミン再取り込み阻害薬」

　　[★]

英

dopamine reuptake inhibitor

関

ドパミン取り込み阻害薬、ドパミン再取り込み阻害剤、ドーパミン取り込み阻害剤

「inhibit」

　　[★]

• v.

• 抑制する、阻害する、阻止する

関

abrogate、block、depress、depression、deter、inhibition、interdict、prevent、prevention、repress、repression、restrain、restraint、suppress、suppression

　 　 　 　

「inhibitor」

　　[★]

• n.

• 阻害剤、阻害薬、抑制薬、抑制剤、(内在性物質について)インヒビター、抑制物質

関

blocker、depressant、suppressant