GABA transaminase inhibitor - Mashpedia, the Real-Time Encyclopedia

A GABA transaminase inhibitor is an enzyme inhibitor that acts upon GABA transaminase.

Examples include vigabatrin,^[1] phenylethylidenehydrazine and ethanolamine-O-sulfate (EOS).

Certain members of this class are used as anticonvulsants.

There is some evidence that Melissa officinalis (lemon balm) inhibits GABA transaminase.^[2]

References [edit]

^ Wang QP, Jammoul F, Duboc A, et al (April 2008). "Treatment of epilepsy: the GABA-transaminase inhibitor, vigabatrin, induces neuronal plasticity in the mouse retina". Eur. J. Neurosci. 27 (8): 2177–87. doi:10.1111/j.1460-9568.2008.06175.x. PMC 2933832. PMID 18412635.
^ http://www.ingentaconnect.com/content/nrc/cjpp/2007/00000085/00000009/art00015

GABA_A	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 GABA_A receptor PAMs navbox for a full list of GABA_A 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

GABA_B	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

GABA_C	Agonists: Main site: CACA CAMP GABOB N⁴-Chloroacetylcytosine arabinoside Progabide Tolgabide Antagonists: Main site: Bilobalide TPMPA

Reuptake
inhibitors

Plasmalemmal

GAT inhibitors	CI-966 Deramciclane EF-1502 Gabaculine Guvacine Nipecotic acid NNC 05-2090 SKF-89976A SNAP-5114 Tiagabine

Enzyme
inhibitors

Anabolism

GAD inhibitors	Allylglycine

Catabolism

GABA-T inhibitors	3-Hydrazinopropionic acid Aminooxyacetic acid Gabaculine Isoniazid Phenelzine Phenylethylidenehydrazine Sodium valproate Valnoctamide Valproate pivoxil Valproate semisodium (Divalproex sodium) Valproic acid Valpromide Vigabatrin

Others

Precursors	Glutamate Glutamine

Cofactors	Vitamin B₆ (pyridoxine pyridoxamine pyridoxal phosphate)

Others	Gabapentin Hopantenic acid Picamilon Pregabalin L-Theanine

Anticonvulsants (N03)

GABA_A receptor agonist

Barbiturates	Barbexaclone Metharbital Methylphenobarbital Pentobarbital Phenobarbital^# Primidone

Benzodiazepines	Clobazam Clonazepam Clorazepate Diazepam^# Flutoprazepam Lorazepam Midazolam Nimetazepam Nitrazepam Temazepam

Other GABA agents

Aromatic allylic alcohols	Stiripentol

Carbonic anhydrase inhibitor

Sulfa drugs	Acetazolamide Ethoxzolamide Sultiame Topiramate Zonisamide

Channel blockers

Primarily sodium

Hydantoins	Ethotoin Fosphenytoin Mephenytoin Phenytoin^#

Carboxamides	Carbamazepine^# Eslicarbazepine acetate Oxcarbazepine Oxitriptyline Rufinamide

Primarily calcium

Succinimides	Ethosuximide^# Mesuximide Phensuximide

AMPA receptor

Perampanel

Unknown/ungrouped

Phenyltriazine (Lamotrigine), Oxazolidinediones (Ethadione
Paramethadione
Trimethadione), Ureas (Phenacemide
Pheneturide), Monosaccharide (Topiramate)

Channel openers

Potassium	Retigabine

Indirect GABA agents

Carboxylic acids/ Fatty acid derivatives	GABA transaminase inhibitor: Valproic acid^# (Sodium valproate & Valproate semisodium) Valpromide Valnoctamide Valproate pivoxil GABA reuptake inhibitor: Tiagabine

GABA analogs	Gabapentin Pregabalin Progabide Tolgabide Vigabatrin

Unknown/multiple/
unsorted

Carbamates	Emylcamate Felbamate Meprobamate Carisbamate

Pyrrolidines	Brivaracetam Levetiracetam Nefiracetam Seletracetam

Propionates	Beclamide Lacosamide

Aldehydes	Paraldehyde

Bromides	Potassium bromide Sodium bromide

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: CNS

anat (n/s/m/p/4/e/b/d/c/a/f/l/g)/phys/devp

noco (m/d/e/h/v/s)/cong/tumr, sysi/epon, injr

proc, drug (N1A/2AB/C/3/4/7A/B/C/D)

Pharmacology: enzyme inhibition

Class

Substrate

Oxidoreductase (EC 1)	1.1 Aldose reductase HMG-CoA reductase 1.3 5-alpha-reductase 1.4 Monoamine oxidase 1.5 Dihydrofolate reductase 1.13 Lipoxygenase 1.14 Aromatase COX-2 1.17 Xanthine oxidase Ribonucleotide reductase

Transferase (EC 2)	2.1 COMT Thymidylate synthase 2.4 PARP 2.5 Dihydropteroate synthetase Farnesyltransferase 2.6 GABA transaminase 2.7 Nucleotidyltransferase Integrase Reverse transcriptase Protein kinase Tyrosine-kinase Janus kinase

Hydrolase (EC 3)	3.1 Phosphodiesterase Acetylcholinesterase Ribonuclease 3.2 Polygalacturonase Neuraminidase Alpha-glucosidase 3.4 Protease: Exopeptidase Dipeptidyl peptidase-4 ACE Endopeptidase Trypsin Renin Matrix metalloproteinase 3.5 Histone deacetylase Beta-lactamase

Lyase (EC 4)	4.1 Dopa decarboxylase 4.2 Carbonic anhydrase