- 関
- GABA agent、GABAergic drug
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)
PrepTutorEJDIC
- General Admiral / (またGa)Georgia
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/11 00:13:30」(JST)
[Wiki en表示]
A GABA agonist is a drug which acts to stimulate or increase the action at the GABA receptor, producing typically sedative effects, and may also cause other effects such as anxiolytic and muscle relaxant effects. There are three receptors of the gamma-aminobutyric acid. The two receptors GABA-α and GABA-ρ are ion channels that signal chloride and diminish further action potentials. The GABA-β receptor belongs to the class of G-Protein coupled receptors that inhibit adenylyl cyclase, therefore leading to decreased cyclic adenosine monophosphate (cAMP). GABA-α and GABA-ρ receptors produces sedative and hypnotic effects as well as producing anti-convulsion properties. GABA-β receptors also produce sedative effects and also leading to changes in gene transcription.
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Contents
- 1 GABA-α agonists
- 2 GABA-β agonists
- 3 GABA-ρ agonists
- 4 External links
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GABA-α agonists [edit]
- acamprosate
- barbiturates
- benzodiazepines
- ethanol
- methaqualone
- muscimol
- nonbenzodiazepines (zaleplon, zolpidem, zopiclone)
- picamilon
- progabide
- tiagabine
GABA-β agonists [edit]
- baclofen
- 1,4-Butanediol
- GBL (γ-Butyrolactone)
- GHB (γ-Hydroxybutyric acid)
- GHV (γ-Hydroxyvaleric acid)
- GVL (γ-Valerolactone)
- lesogaberan
- phenibut
GABA-ρ agonists [edit]
- (Z)-4-Amino-2-butenoic acid
- (+)-cis-2-Aminomethylcyclopropane carboxylic acid
- N4-Chloroacetylcytosine arabinoside
- GABOB (γ-Amino-beta-hydroxybutyric acid)
- progabide
External links [edit]
- GABA agonists at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82018755
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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 |
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Enzyme
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see Enzyme inhibition
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Ion channel
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- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
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Receptor &
transporter
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BA/M
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Adrenergic
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- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
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Dopaminergic
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- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
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Histaminergic
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- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
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Serotonergic
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- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
- Serotonin reuptake enhancer (SRE)
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AA
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GABAergic
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- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
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Glutamatergic
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- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
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Cholinergic
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- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
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Endocannabinoid
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- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
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Opioid
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- Opioid receptor agonist
- Opioid receptor antagonist
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Other
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- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
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Miscellaneous
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- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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GABAergics
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Receptor
ligands |
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GABAA
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- Agonists: Main site: Bamaluzole
- Gaboxadol
- Ibotenic acid
- Isoguvacine
- Isonipecotic acid
- Muscimol (Amanita Muscaria)
- Progabide
- SL 75102
- Thiomuscimol
- Tolgabide; Positive allosteric modulators: Alcohols (2M2B, Ethanol, Ethchlorvynol, Methylpentynol
- Barbiturates
- Benzodiazepines
- Carbamates
- Chlormezanone
- Clomethiazole
- Etomidate
- Kavalactones (Kava)
- Loreclezole
- Metomidate
- Neuroactive steroids
- Nonbenzodiazepines (β-Carbolines, Cyclopyrrolones, Imidazopyridines, Pyrazolopyrimidines, etc.)
- Phenols
- Piperidinediones
- Propanidid
- Pyrazolopyridines
- Quinazolinones
- ROD-188
- Skullcap
- Stiripentol
- Valerenic acid (Valerian)
Note: See the GABAA receptor PAMs navbox for a full list of GABAA positive allosteric modulators.
- Antagonists: Main site: Bicuculline
- Gabazine
- Pitrazepin
- Quisqualamine; Negative allosteric modulators: 17-Phenylandrostenol (17-PA)
- α5IA
- Bilobalide
- Cicutoxin
- Cyclothiazide
- DMCM
- Flumazenil
- Flurothyl
- Furosemide
- Iomazenil (123I)
- L-655,708
- Oenanthotoxin
- Penicillin
- Pentylenetetrazol
- Picrotoxin
- PWZ-029
- Radequinil
- Ro15-4513
- Sarmazenil
- Suritozole
- Terbequinil
- Thujone
- Thiocolchicoside
- ZK-93426
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GABAB
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- Agonists: Main site: 1,4-Butanediol
- Baclofen
- GBL
- GHB
- GHV
- GVL
- Lesogaberan
- Phenibut
- Progabide
- SKF-97,541
- Tolgabide; Positive allosteric modulators: BHF-177
- BHFF
- BSPP
- CGP-7930
- GS-39783
Antagonists: Main site: CGP-35348
- Phaclofen
- Saclofen
- SCH-50911
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GABAC
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- Agonists: Main site: CACA
- CAMP
- GABOB
- N4-Chloroacetylcytosine arabinoside
- Progabide
- Tolgabide
Antagonists: Main site: Bilobalide
- TPMPA
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Reuptake
inhibitors |
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Plasmalemmal
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GAT inhibitors
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- CI-966
- Deramciclane
- EF-1502
- Gabaculine
- Guvacine
- Nipecotic acid
- NNC 05-2090
- SKF-89976A
- SNAP-5114
- Tiagabine
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Enzyme
inhibitors |
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Anabolism
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Catabolism
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GABA-T inhibitors
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- 3-Hydrazinopropionic acid
- Aminooxyacetic acid
- Gabaculine
- Isoniazid
- Phenelzine
- Phenylethylidenehydrazine
- Sodium valproate
- Valnoctamide
- Valproate pivoxil
- Valproate semisodium (Divalproex sodium)
- Valproic acid
- Valpromide
- Vigabatrin
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| Others |
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Precursors
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Cofactors
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- Vitamin B6 (pyridoxine
- pyridoxamine
- pyridoxal phosphate)
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Others
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- Gabapentin
- Hopantenic acid
- Picamilon
- Pregabalin
- L-Theanine
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Hypnotics/sedatives (N05C)
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GABAA
agonists/PAMs |
Alcohols: 2M2B • Chloralodol • Ethanol (Alcohol) • Ethchlorvynol • Methylpentynol • Trichloroethanol
Barbiturates: Allobarbital • Amobarbital • Aprobarbital • Barbital • Butabarbital • Butobarbital • Cyclobarbital • Ethallobarbital • Heptabarb • Hexobarbital • Mephobarbital • Methohexital • Pentobarbital • Phenallymal • Phenobarbital • Propylbarbital • Proxibarbal • Reposal • Secobarbital • Talbutal • Thiamylal • Thiopental • Vinbarbital • Vinylbital
Benzodiazepines: Brotizolam • Clonazepam • Cinolazepam • Climazolam • Doxefazepam • Estazolam • Flunitrazepam • Flurazepam • Flutoprazepam • Haloxazolam • Loprazolam • Lorazepam •Lormetazepam • Midazolam • Nimetazepam • Nitrazepam • Quazepam • Temazepam • Triazolam
Carbamates: Carisoprodol • Ethinamate • Hexapropymate • Meprobamate • Methocarbamol • Procymate • Tybamate
Neuroactive Steroids: Acebrochol • Allopregnanolone • Alphadolone • Alphaxolone • Eltanolone • Ganaxolone • Hydroxydione • Minaxolone • Org 20599 • Org 21465 • Tetrahydrodeoxycorticosterone
Nonbenzodiazepines: CL-218,872 • Eszopiclone • Indiplon • JM-1232 • Lirequinil • Necopidem • Pazinaclone • ROD-188 • Saripidem • Suproclone • Suriclone • SX-3228 • U-89843A • U-90042 • Zaleplon • Zolpidem • Zopiclone
Phenols: Fospropofol • Propofol
Piperidinediones: Glutethimide • Methyprylon • Pyrithyldione • Piperidione
Quinazolinones: Afloqualone • Cloroqualone • Diproqualone • Etaqualone • Mebroqualone • Mecloqualone • Methaqualone • Methylmethaqualone • Nitromethaqualone • SL-164
Volatiles/gases: • Acetophenone • Acetylglycinamide chloral hydrate • Centalun • Chloral hydrate • Paraldehyde
Others: Bromide (Lithium bromide, Potassium bromide, Sodium bromide) • Chloralose • Clomethiazole • Dichloralphenazone • Etomidate • Gaboxadol • Loreclezole • Metomidate • Org 25435 • Petrichloral • Sulfonmethane • Triclofos • Valerenic acid (Valerian)
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GABAB
agonists |
1,4-Butanediol • Aceburic acid • GABOB • GHB (Sodium oxybate) • GBL • GVL
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H1 inverse
agonists |
Antihistamines: Captodiame • Cyproheptadine • Diphenhydramine • Doxylamine • Hydroxyzine • Methapyrilene • Pheniramine • Promethazine • Propiomazine
Antidepressants: Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
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α1-Adrenergic
antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Niaprazine
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α2-Adrenergic
agonists |
4-NEMD • Clonidine • Detomidine • Dexmedetomidine • Lofexidine • Medetomidine • Romifidine • Tizanidine • Xylazine
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5-HT2A
antagonists |
Antidepressants: Serotonin antagonists and reuptake inhibitors (Trazodone) • Tricyclic antidepressants (Amitriptyline, Doxepin, Trimipramine, etc.) • Tetracyclic antidepressants (Mianserin, Mirtazapine, etc.)
Antipsychotics: Typical antipsychotics (Chlorpromazine, Thioridazine, etc.) • Atypical antipsychotics (Olanzapine, Quetiapine, Risperidone, etc.)
Others: Eplivanserin • Niaprazine • Pruvanserin • Volinanserin
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Melatonin
agonists |
Agomelatine • LY-156,735 • Melatonin • Ramelteon • Tasimelteon
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Orexin
antagonists |
Almorexant • SB-334,867 • SB-408,124 • SB-649,868 • Suvorexant • TCS-OX2-29
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| Others |
Acecarbromal • Apronal • Bromisoval • Cannabidiol (Cannabis) • Carbromal • Embutramide • Evoxine • Fenadiazole • Gabapentin • Kavalactones (Kava) • Mephenoxalone • Opioids (Oxycodone, Morphine (Opium), etc.) • Passion flower • Scopolamine (Mandrake) • UMB68 • Valnoctamide
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UpToDate Contents
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English Journal
- Inflammatory mediator-induced modulation of GABAA currents in human sensory neurons.
- Zhang XL1, Lee KY1, Priest BT2, Belfer I1, Gold MS3.
- Neuroscience.Neuroscience.2015 Dec 3;310:401-9. doi: 10.1016/j.neuroscience.2015.09.048. Epub 2015 Sep 28.
- The purpose of the present study was to characterize the properties of A-type GABA receptor (GABAA receptor) currents in human sensory neurons. Neurons were obtained from adult organ donors. GABAA currents were recorded in isolated neurons. Both large inactivating low-affinity currents and smaller p
- PMID 26415765
- Alterations in primary motor cortex neurotransmission and gene expression in hemi-parkinsonian rats with drug-induced dyskinesia.
- Lindenbach D1, Conti MM1, Ostock CY1, Dupre KB1, Bishop C2.
- Neuroscience.Neuroscience.2015 Dec 3;310:12-26. doi: 10.1016/j.neuroscience.2015.09.018. Epub 2015 Sep 9.
- Treatment of Parkinson's disease (PD) with dopamine replacement relieves symptoms of poverty of movement, but often causes drug-induced dyskinesias. Accumulating clinical and pre-clinical evidence suggests that the primary motor cortex (M1) is involved in the pathophysiology of PD and that modulatin
- PMID 26363150
- Prelimbic Cortical Injections of a GABA Agonist and Antagonist: In Vivo Quantification of the Effect in the Rat Brain Using [(18)F] FDG MicroPET.
- Parthoens J1, Servaes S2, Verhaeghe J1, Stroobants S1,3, Staelens S4.
- Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging.Mol Imaging Biol.2015 Dec;17(6):856-64. doi: 10.1007/s11307-015-0859-z.
- PURPOSE: We evaluated the glucose metabolism after microinjections of a GABAA antagonist, bicuculline, and a GABAA agonist, muscimol, in the rat prelimbic cortex (PL) by small animal positron emission tomography (μPET).PROCEDURES: Following a microinjection of either 0.5 μl bicuculline (0.1 mg/m
- PMID 25917751
Japanese Journal
- The change of picrotoxin-induced epileptiform discharges to the beta oscillation by carbachol in rat hippocampal slices
- トラゾドン (特集 従来型向精神薬再考 : 従来型薬が使われるのはどのような場合か)
Related Pictures
★リンクテーブル★
[★]
- 英
- GABA agonist、GABAergic drug、GABA agent
- 関
- GABAアゴニスト、GABA系薬物、GABA作動薬、GABA受容体刺激薬
[★]
- 英
- GABA agonist
- 関
- GABAアゴニスト、GABA作用薬、GABA受容体刺激薬
[★]
- 英
- GABA agonist
- 関
- GABA作用薬、GABA作動薬、GABA受容体刺激薬
[★]
- 英
- GABA agonist
- 関
- GABAアゴニスト、GABA作用薬、GABA作動薬
[★]
- 関
- GABA agonist、GABAergic drug
[★]
- butyl
- 英
- γ-aminobutyric acid, γ-aminobutyrate, gamma aminobutyric acid
- 同
- γ-アミノ酪酸、4-アミノ酪酸、γ-アミノ酪酸、γアミノ酪酸、ガンマアミノブチル酸
- 関
- GABA受容体。ブチル
構造
生合成
[★]
[★]