Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P80404 (GABA transaminase)
 786 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A new quinoline derivative, QUAN-0806 (7-hexyloxy-5-phenyl-1,2,4-triazolo[4,3-alpha]quinoline) was tested for anticonvulsant activity using the maximal electroshock seizure (MES) and the rotarod neurotoxicity (Tox) tests in mice. The MES test showed that QUAN-0806 exhibited higher activity (ED50 = 6.5 mg/kg) and lower toxicity (TD50 = 228.2 mg/kg), resulting in a higher protective index (PI = 35.1) than the reference drugs phenytoin, carbamazepin, phenobarbital, and valproate. In addition, QUAN-0806 was found to exhibit significant oral activity against MES-induced seizures with low oral neurotoxicity in mice. 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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PMID:Evaluation of anticonvulsant activity of QUAN-0806 in various murine experimental seizure models. 1943 43

The levels of glutamic acid decarboxylase (GAD) and ?-amino butyric acid-?-oxoglutarate transaminase (GABA-T) have been investigated in the cochlear nucleus and inferior colliculus of the guinea-pig after hemilateral section of the dorsal acoustic stria. Animals were cerebellectomised and the stria on one side cut. Eleven days later the animals were killed and GAD and GABA-T assayed in the respective nuclei. There was no change in the enzyme levels of the inferior colliculi showing no direct GABA-ergic fibres ascending through the stria and terminating in the inferior colliculi. The levels of both GAD and GABA-T in the cochlear nucleus on the operated side decreased significantly. It is concluded that about 30% of the GAD containing terminals in the cochlear nucleus arise from fibres descending through the dorsal acoustic stria. The bulk of the GABA-ergic transmission in the cochlear nucleus is assumed to involve an intrinsic system of short axoned neurones, the majority of which have their nerve endings in the dorsal part of the nucleus.
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PMID:The effect of lesions of the dorsal acoustic stria on the levels of glutamic acid decarboxylase and GABA transaminase in the inferior colliculus and cochlear nucleus of the guinea-pig. 2048 32