ドパミン受容体拮抗薬
WordNet
- a drug that neutralizes or counteracts the effects of another drug
- a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
- 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
PrepTutorEJDIC
- 対立する人,敵対者,競争相手(opponent)
- =sense organ / 受信装置
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/05/17 22:20:39」(JST)
[Wiki en表示]
Dopamine receptor antagonist
Dopaminergic blockers |
Drug class |
Skeletal structor formula of Haloperidol, a typical antipsychotic
|
Use |
Schizophrenia, bipolar disorder, nausea and vomiting, etc. |
Biological target |
Dopamine receptors |
ATC code |
N05A |
External links |
MeSH |
D012559 |
A dopamine antagonist is a drug which blocks dopamine receptors by receptor antagonism. There are five known types of dopamine receptors in the human body; they are found in the brain, peripheral nervous system, blood vessels, gastrointestinal tract[1] and the kidney.
Contents
- 1 Uses and examples
- 2 Side effects
- 3 Examples
- 4 See also
- 5 References
- 6 External links
Uses and examples
Clozapine, a second generation antipsychotic
Dopamine receptor antagonists are used for some diseases such as schizophrenia, bipolar disorder, nausea and vomiting. It can also control the symptoms of hypersexuality and increased orgasmic activity.
Antidopaminergics such as haloperidol can be an antidote for poisoning with cocaine, amphetamines and dopamine agonists such as Bromocriptine and/or Ropinirole.
- Agents such as atypical antipsychotics (coupled with serotonin antagonist effects): paliperidone, clozapine, risperidone, olanzapine, quetiapine, and ziprasidone
- Used as antiemetics: metoclopramide, droperidol, domperidone
- Used as tricyclic antidepressants: amoxapine, clomipramine, trimipramine
Side effects
They may include one or more of the following and last indefinitely even after cessation of the dopamine antagonist, especially after long-term or high-dosage use:
- Anxiety disorders (such as social phobia)
- Dysphoria and clinical depression
- Extrapyramidal symptoms, including:
- Akathisia
- Parkinsonism due to effects on the nigrostriatal pathway
- Tardive dyskinesia (long-term use)
- Galactorrhea due to removal of dopamine-mediated inhibition of prolactin release from lactotroph cells in the anterior pituitary
- Hyperprolactinaemia due to effects on the tuberoinfundibular pathway
- Increased appetite
- Irritability and aggression
- Low libido, sexual dysfunction and impotence due to blockage of the pleasure center (dopaminergic pathways)
- Menstrual disorder
- Metabolic changes with increased risk of obesity and diabetes mellitus type 2
- Neuroleptic Induced Deficit Syndrome (long-term use)
- Paranoia (rare)[citation needed]
- Sedation or psychomotor agitation
- Symptoms similar to ADHD
- Symptoms similar to narcolepsy
Examples
Examples of Dopamine antagonists include:[2]
- acepromazine
- amisulpride
- amoxapine
- azaperone
- benperidol
- bromopride
- butaclamol
- clomipramine (mild)
- chlorpromazine
- chlorprothixene
- clopenthixol
- domperidone
- droperidol
- eticlopride
- flupenthixol
- fluphenazine
- fluspirilene
- haloperidol
- hydroxyzine
- iodobenzamide
- loxapine
- mesoridazine
- levomepromazine
- metoclopramide
- nafadotride
- nemonapride
- olanzapine
- paliperidone
- penfluridol
- perazine
- perphenazine
- pimozide
- prochlorperazine
- promazine
- quetiapine
- raclopride
- remoxipride
- risperidone
- spiperone
- spiroxatrine
- stepholidine
- sulpiride
- sultopride
- tetrahydropalmatine
- thiethylperazine
- thioridazine
- thiothixene
- tiapride
- trifluoperazine
- trifluperidol
- triflupromazine
- ziprasidone
See also
- Dopamine agonist
- Dopaminergic
- Serotonin antagonist
- Adrenergic antagonist
- Histamine antagonist
- Acetylcholine antagonist
- GABA antagonist
References
- ^ http://www.experts.umich.edu/grantDetail.asp?t=ep1&id=2680068&o_id=&n=Bitar%2C+Khalil+N&u_id=1335
- ^ MeSH list of agents 82018492
External links
- Dopamine antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
Dopaminergics
|
|
Receptor ligands
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|
DR
|
- 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-86929
- Adrogolide (ABT-431, DAS-431)
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine; Others: A-68930
- A-77636
- A-412997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Bifeprunox
- BP-897
- Captodiame
- 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
|
|
|
|
Transporter modulators
|
|
DAT
|
|
|
VMATs
|
- Inhibitors: Amiodarone
- Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
- APP
- AZIK
- Bietaserpine
- Deserpidine
- Dihydrotetrabenazine
- Efavirenz
- GBR-12935
- GZ-793A
- Ibogaine
- Ketanserin
- Lobeline
- Methoxytetrabenazine
- NBI-98854
- Reserpine
- Rose bengal
- SD-809
- Tetrabenazine
- Vanoxerine (GBR-12909)
|
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Enzyme inhibitors
|
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PAH
|
|
|
TH
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
AAAD
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
MAO
|
- 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
- Ladostigil
- Lazabemide
- Milacemide
- Nicotine
- Pargyline‡
- Rasagiline
- Safinamide
- Selegiline (L-deprenyl)
|
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COMT
|
- Entacapone
- Nitecapone
- Opicapone
- Tolcapone
|
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DBH
|
- 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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Neurotoxins
|
- Amphetamine
- DMDHIQ+
- Methamphetamine
- MPP+
- MPTP
- NMDHIQ+
- NMNorsal (2-MDTIQ)
- NMSal
- Norsalsolinol
- Oxidopamine (6-OHDA)
- Rotenone
- Salsolinol
|
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Others
|
- Activity enhancers: BPAP
- PPAP; Levodopa prodrugs: XP21279
|
|
|
|
See also: Adrenergics • Melatonergics • Serotonergics • List of dopaminergic drugs
|
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Neuromodulation
|
|
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
|
|
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)
|
|
Histaminergic
|
- 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)
|
|
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AA
|
GABAergic
|
- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
|
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Glutamatergic
|
- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
- Glutamate reuptake inhibitor
|
|
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Cholinergic
|
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
|
|
Endocannabinoid
|
- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
|
|
Opioidergic
|
- Opioid modulator
- Opioid receptor agonist
- Opioid receptor antagonist
|
|
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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Drugs for functional gastrointestinal disorders (A03)
|
|
Drugs for
functional
bowel disorders |
Antimuscarinics
|
Tertiary
amino group
|
- Oxyphencyclimine
- Camylofin
- Mebeverine
- Trimebutine
- Rociverine
- Dicycloverine
- Dihexyverine
- Difemerine
- Piperidolate
|
|
Quaternary
ammonium
compounds
|
- Benzilone
- Mepenzolate
- Pipenzolate
- Glycopyrronium
- Oxyphenonium
- Penthienate
- Methantheline
- Propantheline
- Otilonium
- Tridihexethyl
- Isopropamide
- Hexocyclium
- Poldine
- Bevonium
- Diphemanil
- Tiemonium
- Prifinium
- Timepidium
- Fenpiverinium
|
|
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Phosphodiesterase
inhibitors
|
- Papaverine
- Drotaverine
- Moxaverine
|
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Acting on
serotonin receptors
|
- 5-HT3 antagonists
- 5-HT4 agonists
- Mosapride
- Prucalopride
- Tegaserod
|
|
Other
|
- Alverine
- Caroverine
- Chlorbenzoxamine
- Diisopromine
- Dimethylaminopropionylphenothiazine
- Fenpiprane
- Fenoverine
- Idanpramine
- Isometheptene
- Phloroglucinol
- Pinaverium
- Proxazole
- Silicones
- Tiropramide
- Trepibutone
- Trimethyldiphenylpropylamine
|
|
|
Belladonna
and derivatives
(antimuscarinics) |
- tertiary amines: Atropine
- Hyoscyamine
- quaternary ammonium compounds:
- Scopolamine
- Butylscopolamine
- Methylscopolamine
- Methylatropine
- Fentonium
- Cimetropium bromide
|
|
Propulsives |
- primarily dopamine antagonists
- Metoclopramide/Bromopride
- Clebopride
- Domperidone
- Alizapride
- 5-HT4 agonists
|
|
Index of digestion
|
|
Description |
- Anatomy
- Physiology
- Development
|
|
Disease |
- Congenital
- Neoplasms and cancer
- Inflammatory bowel disease
- Gluten sensitivity
- Other
- Symptoms and signs
- Blood tests
|
|
Treatment |
- Procedures
- Drugs
- anabolic steroids
- antacids
- diarrhoea and infection
- bile and liver
- functional gastrointestinal disorders
- laxatives
- peptic ulcer and reflux
- nausea and vomiting
- other
- Surgery
|
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UpToDate Contents
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English Journal
- Role of the D3 dopamine receptor in nicotine sensitization.
- Smith LN1, Bachus SE2, McDonald CG2, Smith RF2.
- Behavioural brain research.Behav Brain Res.2015 Aug 1;289:92-104. doi: 10.1016/j.bbr.2015.04.025. Epub 2015 Apr 20.
- Adolescent cigarette use is associated with reduced quitting success and continued smoking in adulthood. Interestingly, polymorphisms of the dopamine D3 receptor (DRD3) gene have been associated with smoking behavior, and the receptor is expressed in an age- and brain region-dependent manner that su
- PMID 25907750
- Neuroprotection in Parkinsonian-treated mice via estrogen receptor α activation requires G protein-coupled estrogen receptor 1.
- Bourque M1, Morissette M2, Di Paolo T3.
- Neuropharmacology.Neuropharmacology.2015 Aug;95:343-52. doi: 10.1016/j.neuropharm.2015.04.006. Epub 2015 Apr 17.
- We have previously shown that estrogen receptors (ER) α activation and G protein-coupled estrogen receptor 1 (GPER1) stimulation reproduce 17β-estradiol protection against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine induced toxicity of dopamine neurons in mice. This suggests that both ERα and GP
- PMID 25892506
- Serotonin6 receptors in the dorsal hippocampus regulate depressive-like behaviors in unilateral 6-hydroxydopamine-lesioned Parkinson's rats.
- Liu KC1, Li JY1, Tan HH2, Du CX2, Xie W3, Zhang YM3, Ma WL1, Zhang L4.
- Neuropharmacology.Neuropharmacology.2015 Aug;95:290-8. doi: 10.1016/j.neuropharm.2015.03.031. Epub 2015 Apr 9.
- Preclinical studies indicate both activation and blockade of serotonin6 (5-HT6) receptors may produce antidepressant-like effects. Depression is a common symptom in Parkinson's disease (PD); however, its pathophysiology is unclear. Here we examined whether 5-HT6 receptors in the dorsal hippocampus (
- PMID 25863121
Japanese Journal
- Antidepressant-Like Effects of Sanggenon G, Isolated from the Root Bark of Morus alba, in Rats: Involvement of the Serotonergic System
Related Links
- Dopamine receptor antagonist Dopaminergic blockers Drug class Skeletal structor formula of Haloperidol, a typical antipsychotic Use Schizophrenia, bipolar disorder, nausea and vomiting, etc. Biological target Dopamine receptors ...
- Dopamine receptor antagonists As peripheral and central dopaminergic receptors are rather similar, the specificity of action of an antagonist on peripheral or central receptors depends primarily on its pharmacokinetic features. If ...
Related Pictures
★リンクテーブル★
[★]
- 英
- dopamine antagonist、dopaminergic antagonist, dopamine receptor antagonist
- 同
- ドパミン受容体拮抗薬、ドパミン受容体遮断薬、ドパミン拮抗薬、ドパミン遮断薬、抗ドパミン薬 antidopaminergic agent
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