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

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/03/13 18:42:04」(JST)

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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.

Uses[edit]

Dopamine

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[edit]

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[edit]

Examples of dopamine agonists include:

Partial agonist[edit]

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 K_i=5-10nM and EC₅₀=50-90nM)^[5]

Agonists of full/unknown efficacy[edit]

Adderall(ADHD stimulant drug)
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)
Dextroamphetamine/Dexedrine (ADHD stimulant drug)
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)
Methylphenidate (Ritalin) (ADHD stimulant drug,has also been used in treatment of Parkinson's disease)^[7]
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)
Lisdexamphetamine (Vyvanse) (First-ever ADHD stimulant Pro-drug)^[8]

Some, such as fenoldopam, are selective for dopamine receptor D1.^[9]

References[edit]

^ 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
^ http://www.ohsu.edu/xd/about/news_events/news/2004/05-6-ritalin-may-improve-parki.cfm
^ http://www.ncbi.nlm.nih.gov/pubmed/18518785
^ 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[edit]

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

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
2. 高プロラクチン血症のマネージメント management of hyperprolactinemia
3. 成人におけるむずむず脚症候群／Willis-Ekbom病の治療 treatment of restless legs syndrome willis ekbom disease in adults
4. 周産期心筋症：治療および予後 peripartum cardiomyopathy treatment and prognosis
5. 排卵誘発の概要 overview of ovulation induction

English Journal

Phosphodiesterase 10A controls D1-mediated facilitation of GABA release from striato-nigral projections under normal and dopamine-depleted conditions.

Mango D, Bonito-Oliva A, Ledonne A, Nisticò R, Castelli V, Giorgi M, Sancesario G, Fisone G, Berretta N, Mercuri NB.SourceIRCCS Fondazione Santa Lucia, Rome, Italy; Department of Systems Medicine, University of Rome Tor Vergata, Rome, Italy.
Neuropharmacology.Neuropharmacology.2014 Jan;76 Pt A:127-36. doi: 10.1016/j.neuropharm.2013.08.010. Epub 2013 Aug 22.
In the present study, we found that PDE10A inhibitor papaverine, alone or in combination with the D1 receptor agonist SKF38393, did not change spontaneous IPSCs (sIPSCs) frequency or amplitude in the substantia nigra pars reticulata (SNpr). An increase in frequency, but not in amplitude, of sIPSCs w
PMID 23973317

Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive decline.

Kauser H, Sahu S, Kumar S, Panjwani U.SourceDefence Institute of Physiology and Allied Sciences (DIPAS), Defence Research and Development Organization (DRDO), Lucknow Road, Timarpur, Delhi 110 054, India.
Neuroscience.Neuroscience.2013 Dec 19;254:110-9. doi: 10.1016/j.neuroscience.2013.09.023. Epub 2013 Sep 18.
Hypobaric hypoxia (HH), an environmental stress resulting from ascent to high altitude, affects perception, memory, judgment, and attention, resulting in degradation of many aspects of normal functioning. Alpha 2A adrenergic agonist, guanfacine proved to be beneficial in the amelioration of neurolog
PMID 24056194

l-Isocorypalmine reduces behavioral sensitization and rewarding effects of cocaine in mice by acting on dopamine receptors.

Xu W, Wang Y, Ma Z, Chiu YT, Huang P, Rasakham K, Unterwald E, Lee DY, Liu-Chen LY.SourceCenter for Substance Abuse Research and Department of Pharmacology, Temple University School of Medicine, 3500 North Broad Street, Philadelphia, PA 19140, USA.
Drug and alcohol dependence.Drug Alcohol Depend.2013 Dec 1;133(2):693-703. doi: 10.1016/j.drugalcdep.2013.08.021. Epub 2013 Sep 2.
BACKGROUND: We previously reported isolation of l-isocorypalmine (l-ICP), a mono-demethylated analog of l-tetrahydropalmatine (l-THP), from the plant Corydalis yanhusuo. Here we characterized its in vitro pharmacological properties and examined its effects on cocaine-induced behaviors in mice.METHOD
PMID 24080315

Japanese Journal

症例報告 ART治療における卵巣過剰刺激症候群に対するCabergolineの予防効果の検討

三宅達也,筒井建紀,正木秀武 [他]
産婦人科の進歩 67(3), 270-275, 2015-08
NAID 40020554977

起床困難に対する自己覚醒技法と薬物療法(研究発表,第39回生命情報科学シンポジウム)

中島亨,戸部有希子
Journal of International Society of Life Information Science 33(1), 80, 2015-03-01
NAID 110009919512

先端巨大症の治療戦略

富永篤,木下康之,栗栖薫
脳神経外科ジャーナル 24(8), 521-527, 2015
… そのほかにdopamine agonistやGH receptor antagonistが用いられる. … Dopamine agonistは内服薬であるが有効率は低い. …
NAID 130005094985

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リンク元

「ドパミン作動薬」

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

　　[★]

英: dopamine agonist、dopaminergic agonist、dopaminergic agent, dopaminergic drug, dopamine receptor agonist, dopamine receptor stimulant
同: ドパミン作用薬、ドパミン刺激薬、ドパミン受容体作用薬、ドパミン受容体作動薬、ドパミン受容体刺激薬、ドパミンアゴニスト
関: ドパミン

[show details]

ドパミン受容体刺激薬 : 約 19,800 件
ドパミン受容体作動薬 : 約 30,900 件
ドパミン受容体作用薬 : 69 件
ドパミン刺激薬 : 52 件
ドパミン作動薬 : 約 91,100 件
ドパミン作用薬 : 約 10,100 件

ドパミン作動薬：レボドパ、ブロモクリプチン、インスリン、アルギニン、グルカゴン、プロプラノール(QB.D-254)

[1] ClinicalTrials.gov NCT00334048 - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"

[2] 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.

[3] "MedlinePlus Drug Information: Pramipexole (Systemic)". United States National Library of Medicine. Archived from the original on 2006-09-26. Retrieved 2006-09-27.

[4] 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.

[5] 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.

[6] FDA Announces Voluntary Withdrawal of Pergolide Products

[7] ttp://www.ohsu.edu/xd/about/news_events/news/2004/05-6-ritalin-may-improve-parki.cfm

[8] ttp://www.ncbi.nlm.nih.gov/pubmed/18518785

[pmid10696081-9] 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.

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dopamine agonist