ドパミン作動薬
WordNet
- (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
- a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
- someone involved in a contest or battle (as in an agon)
- 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
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/06/15 02:01:12」(JST)
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Dopamine Receptor agonist |
Drug class |
Use |
Parkinson's disease, Attention deficit/hyperactivity disorder(ADHD), restless legs syndrome, clinical depression, etc. |
Biological target |
Dopamine receptors |
ATC code |
N04 |
External links |
MeSH |
D010300 |
A dopamine agonist is a compound that activates dopamine receptors in the absence of dopamine. Dopamine agonists activate signaling pathways through the dopamine receptor and trimeric G-proteins, ultimately leading to changes in gene transcription.
Contents
- 1 Uses
- 2 Side-effects
- 3 Examples
- 3.1 Partial agonist
- 3.2 Agonists of full/unknown efficacy
- 4 See also
- 5 References
- 6 External links
Uses
More examples are found in main articles of DA examples
Some medical drugs act as dopamine agonists and can treat hypodopaminergic (low dopamine) conditions; they are typically used for treating Parkinson's disease, attention deficit/hyperactivity disorder (in the form of stimulants) and certain pituitary tumors (prolactinoma), and may be useful for restless legs syndrome (RLS). Both Requip (Ropinirole) and Mirapex (Pramipexole) are FDA-approved for the treatment of RLS. There is also an ongoing clinical trial to test the effectiveness of the dopamine agonist Requip (ropinirole) in reversing the symptoms of SSRI-induced sexual dysfunction and Post-SSRI sexual dysfunction (PSSD).[1] Additionally, a systematic review and meta-analysis concluded that prophylactic treatment with cabergoline reduces the incidence, but not the severity, of ovarian hyperstimulation syndrome (OHSS), without compromising pregnancy outcomes, in females undergoing stimulated cycles of in vitro fertilization (IVF).[2]
Side-effects
Some of the common side effects of dopamine agonists include:[3][4]
- Euphoria
- Pericardial effusion
- Fibrous thickening of lining that covers some of the internal organs including the heart or the lungs (fibrotic reaction)
- Hallucinations
- Causing or worsening psychosis
- Orthostatic hypotension
- Increased orgasmic intensity
- Weight loss
- Anorexia (symptom)
- Nausea and possible vomiting
- Insomnia
- Unusual tiredness or weakness
- Dizziness
- Drowsiness
- Possible Narcolepsy manifestations (Sleep attacks)
- Lightheadedness
- Raynaud's phenomenon (common side effect of ergot derivatives)
- Syncope
- Twitching, twisting, or other unusual body movements
- Pathological addiction (gambling, shopping, internet pornography, hyper-sexuality) – specifically D3-preferring agonists
Examples
Examples of dopamine agonists include:
Partial agonist
- Aripiprazole (Partial agonist of the D2 family receptors - Trade name "Abilify" in the United States; atypical antipsychotic)
- Phencyclidine (a.k.a. PCP; partial agonist. Psychoactivity mainly due to NMDA antagonism)
- Quinpirole (Partial agonist of the D2 and D3 family of receptors)
- Salvinorin A (chief active constituent of the psychedelic herb salvia divinorum, the psychoactivity of which is mainly due to Kappa-opioid receptor agonism; partial agonist at the D2 with an Intrinsic activity of 40-60%, binding affinity of Ki=5-10nM and EC50=50-90nM)[5]
Agonists of full/unknown efficacy
- Apomorphine (Apokyn) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Bromocriptine (Parlodel) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Cabergoline (Dostinex) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Ciladopa (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Dihydrexidine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Dinapsoline (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Doxanthrine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Epicriptine (Similar to those of Bromocriptine) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Lisuride (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Pergolide (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Permax) - Removed from the market in the USA March 29, 2007.[6]
- Piribedil (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Pramipexole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Mirapex and Sifrol)
- Propylnorapomorphine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Quinagolide (Norprolac) (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Ropinirole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Requip)
- Rotigotine (Dopamine Agonist for Parkinson's disease/Restless leg syndrome) (Neupro)
- Roxindole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
- Sumanirole (Dopamine Agonist for Parkinson's disease/Restless leg syndrome)
Some, such as fenoldopam, are selective for dopamine receptor D1.[7]
See also
- Dopamine antagonist
- Receptor agonist
- Dopaminergic
- Serotonin agonist
- Adrenergic agonist (Sympathomimetic)
- Histamine agonist
- Acetylcholine agonist (Parasympathomimetic)
- GABA agonist
References
- ^ ClinicalTrials.gov NCT00334048 - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
- ^ Youssef MA, van Wely M, Hassan MA, et al. (March 2010). "Can dopamine agonists reduce the incidence and severity of OHSS in IVF/ICSI treatment cycles? A systematic review and meta-analysis". Hum Reprod Update 16 (5): 459–66. doi:10.1093/humupd/dmq006. PMID 20354100.
- ^ "MedlinePlus Drug Information: Pramipexole (Systemic)". United States National Library of Medicine. Archived from the original on 2006-09-26. Retrieved 2006-09-27.
- ^ Boyd, Alan (1995). "Bromocriptine and psychosis: A literature review". Psychiatric Quarterly 66 (1): 87–95. doi:10.1007/BF02238717. PMID 7701022. Retrieved 2008-09-06.
- ^ Seeman P, Guan HC, Hirbec H (2009). "Dopamine D2High receptors stimulated by phencyclidines, lysergic acid diethylamide, salvinorin A, and modafinil". Synapse 63 (8): 698–704. doi:10.1002/syn.20647. PMID 19391150.
- ^ FDA Announces Voluntary Withdrawal of Pergolide Products
- ^ Ng SS, Pang CC (March 2000). "In vivo venodilator action of fenoldopam, a dopamine D(1)-receptor agonist". Br. J. Pharmacol. 129 (5): 853–8. doi:10.1038/sj.bjp.0703119. PMC 1571905. PMID 10696081.
6. Avanzi M, Uber E, Bonfa F. Pathological gambling in two patients on dopamine replacement therapy for Parkinson’s disease. Neurol Sci 2004; 25:98–101[Medline]
External links
- Dopamine Agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- http://www.abc.net.au/news/stories/2008/01/22/2143502.htm
- http://neuro.psychiatryonline.org/cgi/content/full/19/4/473
Dopaminergics
|
|
Receptor ligands
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Agonists
|
- Adamantanes: Amantadine
- Memantine
- Rimantadine; Aminotetralins: 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232; Benzazepines: 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959; Ergolines: Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide; Dihydrexidine derivatives: 2-OH-NPA
- A-86,929
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine; Others: A-68,930
- A-77636
- A-412,997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Bifeprunox
- BP-897
- CY-208,243
- Dizocilpine
- Etilevodopa
- Flibanserin
- Ketamine
- Melevodopa
- Modafinil
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Rotigotine
- Roxindole
- Salvinorin A
- SKF-89,145
- Sumanirole
- Terguride
- Umespirone
- WAY-100,635
|
|
Antagonists
|
- Typical antipsychotics: Acepromazine
- Azaperone
- Benperidol
- Bromperidol
- Clopenthixol
- Chlorpromazine
- Chlorprothixene
- Droperidol
- Flupentixol
- Fluphenazine
- Fluspirilene
- Haloperidol
- Levosulpiride
- Loxapine
- Mesoridazine
- Methotrimeprazine
- Nemonapride
- Penfluridol
- Perazine
- Periciazine
- Perphenazine
- Pimozide
- Prochlorperazine
- Promazine
- Sulforidazine
- Sulpiride
- Sultopride
- Thioridazine
- Thiothixene
- Trifluoperazine
- Triflupromazine
- Trifluperidol
- Zuclopenthixol; Atypical antipsychotics: Amisulpride
- Asenapine
- Blonanserin
- Cariprazine
- Carpipramine
- Clocapramine
- Clorotepine
- Clozapine
- Gevotroline
- Iloperidone
- Lurasidone
- Melperone
- Molindone
- Mosapramine
- Olanzapine
- Paliperidone
- Perospirone
- Piquindone
- Quetiapine
- Remoxipride
- Risperidone
- Sertindole
- Tiospirone
- Zicronapine
- Ziprasidone
- Zotepine; Antiemetics: AS-8112
- Alizapride
- Bromopride
- Clebopride
- Domperidone
- Metoclopramide
- Thiethylperazine; Others: Amoxapine
- Buspirone
- Butaclamol
- Ecopipam
- EEDQ
- Eticlopride
- Fananserin
- Hydroxyzine
- L-745,870
- Nafadotride
- Nuciferine
- PNU-99,194
- Raclopride
- Sarizotan
- SB-277,011-A
- SCH-23,390
- SKF-83,959
- Sonepiprazole
- Spiperone
- Spiroxatrine
- Stepholidine
- Tetrahydropalmatine
- Tiapride
- UH-232
- Yohimbine
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Reuptake inhibitors
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|
Plasmalemmal
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DAT inhibitors
|
- Piperazines: DBL-583
- GBR-12,935
- Nefazodone
- Vanoxerine; Piperidines: BTCP
- Desoxypipradrol
- Dextromethylphenidate
- Difemetorex
- Ethylphenidate
- Methylnaphthidate
- Methylphenidate
- Phencyclidine
- Pipradrol; Pyrrolidines: Diphenylprolinol
- MDPV
- Naphyrone
- Prolintane
- Pyrovalerone; Tropanes: Altropane
- Brasofensine
- CFT
- Cocaine
- Dichloropane
- Difluoropine
- FE-β-CPPIT
- FP-β-CPPIT
- Ioflupane (123I)
- Iometopane
- RTI-112
- RTI-113
- RTI-121
- RTI-126
- RTI-150
- RTI-177
- RTI-229
- RTI-336
- Tenocyclidine
- Tesofensine
- Troparil
- Tropoxane
- WF-11
- WF-23
- WF-31
- WF-33; Others: Adrafinil
- Armodafinil
- Amfonelic acid
- Amphetamine
- Amineptine
- Benzatropine
- Bromantane
- BTQ
- BTS-74,398
- Bupropion
- Ciclazindol
- Diclofensine
- Dimethocaine
- Diphenylpyraline
- Dizocilpine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- Etybenzatropine
- EXP-561
- Fencamine
- Fencamfamine
- Fezolamine
- Fluorenol
- GYKI-52,895
- Indatraline
- Ketamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Mazindol
- Medifoxamine
- Mesocarb
- Modafinil
- Nefopam
- Nomifensine
- NS-2359
- O-2172
- Pridefrine
- Propylamphetamine
- Radafaxine
- SEP-225,289
- SEP-227,162
- Sertraline
- Sibutramine
- Tametraline
- Tedatioxetine
- Tripelennamine
|
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Vesicular
|
VMAT inhibitors
|
- Deserpidine
- Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
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Allosteric modulators
|
|
- Quinazolinamines: SoRI-9804
- SoRI-20040
- SoRI-20041
|
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Enzyme inhibitors
|
|
Anabolism
|
PAH inhibitors
|
|
|
TH inhibitors
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
AAAD/DDC inhibitors
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
|
Catabolism
|
MAO inhibitors
|
- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- Esuprone
- Harmala alkaloids
- Methylene Blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective: D-Deprenyl
- Ethanol
- L-Deprenyl (Selegiline)
- Ladostigil
- Lazabemide
- Milacemide
- Nicotine
- Pargyline
- Rasagiline
- Safinamide
|
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COMT inhibitors
|
- Entacapone
- Nitecapone
- Tolcapone
|
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DBH inhibitors
|
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Tropolone
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Others
|
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Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa)
|
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Cofactors
|
- Ferrous iron (Fe2+)
- Tetrahydrobiopterin
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Others
|
- Activity enhancers: BPAP * PPAP; Toxins: 6-OHDA; Steroids: Anabolic-androgenic steroids
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List of dopaminergic drugs
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Neuromodulation
|
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Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Antagonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- Inverse agonist
- ♦ Transporter [Reuptake]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
|
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Classes |
Enzyme
|
see Enzyme inhibition
|
|
Ion channel
|
- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
|
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Receptor &
transporter
|
BA/M
|
Adrenergic
|
- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
|
|
Dopaminergic
|
- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
|
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Histamitic
|
- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
|
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Serotonergic
|
- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
|
|
|
AA
|
GABAergic
|
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
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Glutamitic
|
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
|
|
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Cholinergic
|
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
|
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Endocannabinoid
|
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
|
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Opioid
|
- Opioid receptor agonist
- Opioid receptor antagonist
|
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Other
|
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
|
|
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Miscellaneous
|
- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
|
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UpToDate Contents
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English Journal
- Selective activation of the trace amine-associated receptor 1 decreases cocaine's reinforcing efficacy and prevents cocaine-induced changes in brain reward thresholds.
- Pei Y1, Mortas P2, Hoener MC2, Canales JJ3.
- Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2015 Dec 3;63:70-5. doi: 10.1016/j.pnpbp.2015.05.014. Epub 2015 Jun 3.
- The newly discovered trace amine-associated receptor 1 (TAAR1) has emerged as a promising target for medication development in stimulant addiction due to its ability to regulate dopamine (DA) function and modulate stimulants' effects. Recent findings indicate that TAAR1 activation blocks some of the
- PMID 26048337
- Effect of dopamine D4 receptor agonists on sleep architecture in rats.
- Nakazawa S1, Nakamichi K2, Imai H2, Ichihara J2.
- Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2015 Dec 3;63:6-13. doi: 10.1016/j.pnpbp.2015.05.006. Epub 2015 May 16.
- Dopamine plays a key role in the regulation of sleep-wake states, as revealed by the observation that dopamine-releasing agents such as methylphenidate have wake-promoting effects. However, the precise mechanisms for the wake-promoting effect produced by the enhancement of dopamine transmission are
- PMID 25985889
- Synthesis and evaluation in rats of homologous series of [(18)F]-labeled dopamine D 2/3 receptor agonists based on the 2-aminomethylchroman scaffold as potential PET tracers.
- Shalgunov V1, van Wieringen JP, Janssen HM, Fransen PM, Dierckx RA, Michel MC, Booij J, Elsinga PH.
- EJNMMI research.EJNMMI Res.2015 Dec;5(1):119. doi: 10.1186/s13550-015-0119-x. Epub 2015 Jul 25.
- BACKGROUND: Agonist positron emission tomography (PET) tracers for dopamine D2/3 receptors (D2/3Rs) offer greater sensitivity to changes in endogenous dopamine levels than D2/3R antagonist tracers. D2/3R agonist tracers currently available for clinical research are labeled with the short-lived isoto
- PMID 26205538
Japanese Journal
- 病気について知りたい! 臨床講座(66)パーキンソン病
- The effect of dopamine on adult hippocampal neurogenesis
- Progress in neuro-psychopharmacology & biological psychiatry 50, 116-124, 2014-04-03
- NAID 120005411146
Related Links
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- What are the facts? Dopamine agonists are a different class of drugs than levodopa. While levodopa is converted in the brain into dopamine, dopamine agonists actually mimic the effects of dopamine without having to be converted. ...