Protein Information

Name GABA transaminase
Synonyms (S) 3 amino 2 methylpropionate transaminase; 4 aminobutyrate aminotransferase; ABAT; ABAT protein; GABA aminotransferase; GABA transaminase; GABA AT; GABA T…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
20109543 Mishra N, Oraon A, Dev A, Jayaprakash V, Basu A, Pattnaik AK, Tripapthi SN, Akhtar M, Ahmad S, Swaroop S, Basu M: Anticonvulsant activity of Benkara malabarica (Linn.) root extract: In vitro and in vivo investigation. J Ethnopharmacol. 2010 Mar 24;128(2):533-6. Epub 2010 Jan 28.

The anticonvulsant activity of the extract was assessed in strychnine-induced and isoniazide-induced convulsion models; phenytoin (20mg/kg) and diazepam (1mg/kg) were used as standards, respectively.
Mechanism of action was studied by performing GABA transaminase (GABA-T) assay, isolated from rat brain.
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19831276 Yogeeswari P, Sriram D, Thirumurugan R, Jeewanlal LR, Jit S, Ragavendran JV, Kavya R, Rakhra K, Saraswat V: Synthesis of N4-(2,4-dimethylphenyl) semicarbazones as 4-aminobutyrate aminotransferase inhibitors. Acta Pharm. 2006 Sep;56(3):259-72.

All the compounds were evaluated for anticonvulsant activity by using a series of test models, including maximal electroshock seizure, subcutaneous pentylenetetrazole and subcutaneous strychnine seizure threshold tests.
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15056857 Koo BS, Lee SI, Ha JH, Lee DU: Inhibitory effects of the essential oil from SuHeXiang Wan on the central nervous system after inhalation. Biol Pharm Bull. 2004 Apr;27(4):515-9.

Preinhalation of the fragrance oil markedly delayed the appearance of pentylenetetrazole-induced convulsion, but showed weak activities on picrotoxin- and strychnine-induced convulsions, which implies this drug may inhibit the convulsion by GABAergic neuromodulation.
Furthermore, inhalation inhibited the activity of GABA transaminase as the inhalation period was lengthened.
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8176438 Trombley PQ, Shepherd GM: Glycine exerts potent inhibitory actions on mammalian olfactory bulb neurons. J Neurophysiol. 1994 Feb;71(2):761-7.

At moderate concentrations (> 1 microM) strychnine nonselectively antagonized both glycine- and GABA-evoked currents.
Similarly, picrotoxin was a nonselective antagonist for glycine- and GABA-mediated currents at high concentrations (100 microM), but was selective for GABA at low concentrations (10 microM).(ABSTRACT TRUNCATED AT 250 WORDS)
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10835046 Lim R, Alvarez FJ, Walmsley B: GABA mediates presynaptic inhibition at glycinergic synapses in a rat auditory brainstem nucleus. J Physiol. 2000 Jun 1;525 Pt 2:447-59.

We have investigated the roles of glycine and GABA at synapses on bushy cells in the rat AVCN, using receptor immunohistochemistry and electrophysiology.
This observation was supported by the effect of strychnine (1 microM), which was to decrease the evoked IPSC (to 10 % of control IPSC amplitude) and to produce a greater than 90 % block of spontaneous miniature IPSCs.
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12957225 Matsumoto K, Nomura H, Murakami Y, Taki K, Takahata H, Watanabe H: Long-term social isolation enhances picrotoxin seizure susceptibility in mice: up-regulatory role of endogenous brain allopregnanolone in GABAergic systems. Pharmacol Biochem Behav. 2003 Jul;75(4):831-5.

Allopregnanolone (ALLO, 3alpha,5alpha-tetrahydroprogesterone), a positive allosteric modulator of actions of gamma-aminobutyric acid GABA) at GABA (A) receptors, is synthesized in the brain from progesterone by the sequential action of two enzymes: a type I 5alpha-reductase and a 3alpha-hydroxysteroid oxidoreductase.
Social isolation of mice for 7 weeks prior to the experiments caused a significant increase of seizure susceptibility to the GABA (A) receptor antagonist picrotoxin but not to the glycine receptor antagonist strychnine or the glutamate receptor agonist kainic acid.
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11082440 Dawson GR, Wafford KA, Smith A, Marshall GR, Bayley PJ, Schaeffer JM, Meinke PT, McKernan RM: Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid (A) receptor. J Pharmacol Exp Ther. 2000 Dec;295(3):1051-60.

Although avermectins weakly inhibited [(3) H] strychnine binding in rat spinal cord, and inhibited glycine responses on primary cultured cortical neurons, activity at glycine receptors did not correlate with either anticonvulsant activity or toxicity.
All the active compounds tested potentiated the effects of GABA at recombinant GABA (A) receptors in oocytes and at native cortical GABA (A) receptors and the efficacy of avermectins at the GABA (A) receptor correlated best with their anticonvulsant potency.
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10980012 Liu QY, Schaffner AE, Chang YH, Maric D, Barker JL: Persistent activation of GABA (A) receptor/Cl (-) channels by astrocyte-derived GABA in cultured embryonic rat hippocampal neurons. J Neurophysiol. 2000 Sep;84(3):1392-403.

ACM induced an increase in cytoplasmic Ca (2+) in cultured embryonic hippocampal neurons that was completely blocked by bicuculline and strychnine.
The baseline current and variance decreased immediately in all cells after either local perfusion with saline or exposure to bicuculline, an antagonist of GABA at GABA (A) receptor/Cl (-) channels.
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8055609 Ries CR, Scoates PJ, Puil E: Opisthotonos following propofol: a nonepileptic perspective and treatment strategy. Can J Anaesth. 1994 May;41(5 Pt 1):414-9.

The preservation of consciousness and similarities to strychnine-induced opisthotonos suggest to us that the mechanism may have a brainstem and spinal origin.
We recommend a therapeutic strategy that restores inhibition by glycine and GABA at multiple sites; the preferred therapeutic agents would be diazepam and physostigmine.
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8004449 Takahashi Y, Shirasaki T, Yamanaka H, Ishibashi H, Akaike N: Physiological roles of glycine and gamma-aminobutyric acid in dissociated neurons of rat visual cortex. Brain Res. 1994 Mar 21;640(1-2):229-35.

Strychnine and bicuculline reversively inhibited both 10 (-5) M GABA- and 10 (-4) M Gly-induced ICl in a concentration-dependent manner.
GABA at 10 (-5) M, which is near the EC50 of the GABA response, induced ICl in all neurons tested (n = 83).
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8584111 Zemkova H, Vanecek J, Krusek J: Electrophysiological characterization of GABAA receptors in anterior pituitary cells of newborn rats. Neuroendocrinology. 1995 Aug;62(2):123-9.

The application of GABA at concentrations 10 microM or higher, induced membrane currents that desensitized.
Inhibition to 56% was observed with 6 microM strychnine.
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19435143 Guan LP, Zhao DH, Jiang Z, Piao HR, Quan ZS: Evaluation of anticonvulsant activity of QUAN-0806 in various murine experimental seizure models. Pharmazie. 2009 Apr;64(4):248-51.

QUAN-0806 was tested in chemically induced models (pentylenetetrazole, PTZ; isoniazid, ISO; 3-mercaptopropionic acid, 3-MPA; and strychnine, STRYC) to further investigate the anticonvulsant activity.
QUAN-0806 produced significant antagonistic activity against seizures induced by PTZ, 3-MPA, and ISO, suggesting that QUAN-0806 influences GABAergic neurotransmission by activating glutamate decarboxylase (GAD) or inhibiting (GABA)-a-oxoglutarate aminotransferase (GABA-T) in the brain.
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10938323 Chery N, De Koninck Y: GABA (B) receptors are the first target of released GABA at lamina I inhibitory synapses in the adult rat spinal cord. J Neurophysiol. 2000 Aug;84(2):1006-11.

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9372227 Karlsson U, Haage D, Johansson S: Currents evoked by GABA and glycine in acutely dissociated neurons from the rat medial preoptic nucleus. Brain Res. 1997 Oct 3;770(1-2):256-60.

GABA, at a concentration of 1 mM, evoked outward currents in all cells (n = 33) when studied at potentials positive to -80 mV.
The currents evoked by glycine were largely blocked by 1 microM strychnine.
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12154171 Mangin JM, Guyon A, Eugene D, Paupardin-Tritsch D, Legendre P: Functional glycine receptor maturation in the absence of glycinergic input in dopaminergic neurones of the rat substantia nigra. J Physiol. 2002 Aug 1;542(Pt 3):685-97.


The application of 1 microM gabazine blocked spontaneous or evoked inhibitory synaptic current, while the addition of 1 microM strychnine had no effect, suggesting a lack of functional glycinergic synapses on DA neurones.
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