HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Evaluation of anticonvulsant activity of QUAN-0806 in various murine experimental seizure models.

Abstract
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.
AuthorsLi-Ping Guan, Dong-Hai Zhao, Zhe Jiang, Hu-Ri Piao, Zhe-Shan Quan
JournalDie Pharmazie (Pharmazie) Vol. 64 Issue 4 Pg. 248-51 (Apr 2009) ISSN: 0031-7144 [Print] Germany
PMID19435143 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 7-hexyloxy-5-phenyl-1,2,4-triazolo(4,3-alpha)quinoline
  • Anticonvulsants
  • Convulsants
  • Quinolines
  • Triazoles
  • gamma-Aminobutyric Acid
  • 4-Aminobutyrate Transaminase
  • Glutamate Decarboxylase
Topics
  • 4-Aminobutyrate Transaminase (metabolism)
  • Animals
  • Anticonvulsants (pharmacokinetics, pharmacology)
  • Brain (drug effects, enzymology)
  • Convulsants (pharmacology)
  • Electroshock
  • Enzyme Activation (drug effects)
  • Female
  • Glutamate Decarboxylase (metabolism)
  • Injections, Intraperitoneal
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Postural Balance (drug effects)
  • Quinolines (pharmacology)
  • Seizures (chemically induced, prevention & control)
  • Synaptic Transmission (drug effects)
  • Triazoles (pharmacology)
  • gamma-Aminobutyric Acid (physiology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: