GABA transaminase inhibitor
A GABA transaminase inhibitor is an enzyme inhibitor that acts upon GABA transaminase.[1]
Examples include valproic acid,[2] vigabatrin,[3][4] phenylethylidenehydrazine, ethanolamine-O-sulfate (EOS), and L-cycloserine.[5]
Certain members of this class are used as anticonvulsants.
There is some evidence that Melissa officinalis (lemon balm), and rosmarinic acid it contains, inhibits GABA transaminase.[6]
References
- ↑ Ciesielski, L.; Simler, S.; Gensburger, C.; Mandel, P.; Taillandier, G.; Benoit-Guyod, J. L.; Boucherle, A.; Cohen-Addad, C.; Lajzerowicz, J. (1979). "GABA transaminase inhibitors". Advances in experimental medicine and biology. Advances in Experimental Medicine and Biology 123: 21–41. doi:10.1007/978-1-4899-5199-1_2. ISBN 978-1-4899-5201-1. PMID 390993.
- ↑ Bruni, J.; Wilder, B. J. (1979). "Valproic acid. Review of a new antiepileptic drug". Archives of neurology 36 (7): 393–398. doi:10.1001/archneur.1979.00500430023002. PMID 110294.
- ↑ 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.
- ↑ Gibson, J. P.; Yarrington, J. T.; Loudy, D. E.; Gerbig, C. G.; Hurst, G. H.; Newberne, J. W. (1990). "Chronic toxicity studies with vigabatrin, a GABA-transaminase inhibitor". Toxicologic pathology 18 (2): 225–238. PMID 2399411.
- ↑ Polc, P.; Pieri, L.; Bonetti, E. P.; Scherschlicht, R.; Moehler, H.; Kettler, R.; Burkard, W.; Haefely, W. (1986). "L-cycloserine: Behavioural and biochemical effects after single and repeated administration to mice, rats and cats". Neuropharmacology 25 (4): 411–418. doi:10.1016/0028-3908(86)90236-4. PMID 3012401.
- ↑ Awad, R.; Levac, D.; Cybulska, P.; Merali, Z.; Trudeau, V. L.; Arnason, J. T. (2007). "Effects of traditionally used anxiolytic botanicals on enzymes of the γ -aminobutyric acid (GABA) systemThis article is one of a selection of papers published in this special issue (part 1 of 2) on the Safety and Efficacy of Natural Health Products". Canadian Journal of Physiology and Pharmacology 85 (9): 933–942. doi:10.1139/Y07-083. PMID 18066140.
GABAergics |
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| Receptor (ligands) | |
- PAMs (abridged; see here for a full list): α-EMTBL
- Alcohols (e.g., ethanol)
- Avermectins (e.g., ivermectin)
- Barbiturates (e.g., phenobarbital)
- Benzodiazepines (e.g., diazepam)
- Bromide compounds (e.g., potassium bromide)
- Carbamates (e.g., meprobamate)
- Carbamazepine
- Chloralose
- Chlormezanone
- Clomethiazole
- Dihydroergolines (e.g., ergoloid (dihydroergotoxine))
- Etazepine
- Etifoxine
- Fenamates (e.g., mefenamic acid)
- Flavonoids (e.g., apigenin, hispidulin)
- Fluoxetine
- Flupirtine
- Imidazoles (e.g., etomidate)
- Kava constituents (e.g., kavain)
- Lanthanum
- Loreclezole
- Monastrol
- Neuroactive steroids (e.g., allopregnanolone, cholesterol)
- Niacin
- Nicotinamide (niacinamide)
- Nonbenzodiazepines (e.g., β-carbolines (e.g., abecarnil), cyclopyrrolones (e.g., zopiclone), imidazopyridines (e.g., zolpidem), pyrazolopyrimidines (e.g., zaleplon))
- Norfluoxetine
- Petrichloral
- Phenols (e.g., propofol)
- Phenytoin
- Piperidinediones (e.g., glutethimide)
- Propanidid
- Pyrazolopyridines (e.g., etazolate)
- Quinazolinones (e.g., methaqualone)
- Retigabine (ezogabine)
- ROD-188
- Skullcap constituents (e.g., baicalin)
- Stiripentol
- Sulfonylalkanes (e.g., sulfonmethane (sulfonal))
- Topiramate
- Valerian constituents (e.g., valerenic acid)
- Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, sevoflurane)
- NAMs: 1,3M1B
- 3M2B
- 17-Phenylandrostenol
- α5IA (LS-193,268)
- β-CCB
- β-CCE
- β-CCM
- β-CCP
- β-EMGBL
- Amiloride
- Anisatin
- β-Lactams (e.g., penicillins, cephalosporins, carbapenems)
- Bemegride
- Bilobalide
- CHEB
- Cicutoxin
- Cloflubicyne
- Cyclothiazide
- DHEA
- DHEA-S
- Dieldrin
- (+)-DMBB
- DMCM
- DMPC
- EBOB
- Etbicyphat
- FG-7142 (ZK-31906)
- Fiproles (e.g., fipronil)
- Flavonoids (e.g., amentoflavone, oroxylin A)
- Flumazenil
- Fluoroquinolones (e.g., ciprofloxacin)
- Flurothyl
- Furosemide
- Iomazenil (123I)
- Isopregnanolone (sepranolone)
- L-655,708
- Laudanosine
- Leptazol
- Lindane
- MaxiPost
- Morphine
- Morphine-3-glucuronide
- MRK-016
- Naloxone
- Naltrexone
- Nicardipine
- Oenanthotoxin
- Pentetrazol (metrazol)
- Phenylsilatrane
- Picrotoxin (i.e., picrotin and picrotoxinin)
- Pregnenolone sulfate
- Propybicyphat
- PWZ-029
- Radequinil
- RG-1662
- Ro 15-4513
- Ro 19-4603
- RO4882224
- RO4938581
- Sarmazenil
- SCS
- Suritozole
- TB-21007
- TBOB
- TBPS
- TCS-1105
- Terbequinil
- TETS
- Thujone
- U-93631
- Zinc
- ZK-93426
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| Transporter (blockers) | |
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| Enzyme (inhibitors) | |
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| Others |
- Others: GABA-T activators: 3-Methyl-GABA
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| See also: GHBergics • Glutamatergics • Glycinergics |
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| GABAergics | |
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| Channelergics | |
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| Others | |
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| Description | |
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| Disorders |
- Mental and behavioral
- Mood
- Developmental
- pervasive
- dyslexia and specific
- Substance-related
- Emotional and behavioral
- Symptoms and signs
- Evaluation and testing
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| Treatment |
- Psychotherapy
- Drugs
- depression
- antipsychotics
- anxiety
- dementia
- hypnotics and sedatives
- psychostimulants, ADHD and nootropics
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