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T. Hámore, S. Sólyom, P. Berzsenyi, F. Andrási and I. Tarnawa, “Structural Analogues of Some Highly active Non-Competitive AMPA Antagonists,” Bioorganic & Medicinal Chemistry Letters, Vol. 10, No. 9, 2000, pp. 899902. doi:10.1016/S0960-894X(00)00117-7

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• TITLE: Synthesis and Evaluation of Anticonvulsant Activity of 6,8-Dimethoxy-3-methyl-1,2,3,4-tetrahydroisoquinoline in PTZ-Induced Seizure Model in Mice

  AUTHORS: Yothawathorn Pariyawongsakul, Chamnan Patarapanich, Chantana Boonyarat, Ploenthip Puthongking

  KEYWORDS: Anticonvulsant; Pentylenetetrazole; Tetrahydroisoquinoline

  JOURNAL NAME: Open Journal of Medicinal Chemistry, Vol.2 No.3, September 27, 2012

  ABSTRACT: This study we describe the synthesis of a novel structure of anticonvulsant agent as 6,8-dimethoxy-3-methyl-1,2,3,4- tetrahydroisoquinoline by using GYKI52466, which was the potent anticonvulsant agent, as the lead molecule. Com-pound IV was synthesized and anticonvulsant effects was evaluated against Pentylenetetrazole (PTZ)-induced seizure model in mice. The acute anticonvulsant effect was tested with a single dose of 25 and 75 µmol/kg of the synthesis compound. Sodium valproate and normal saline were used as the reference standard and control, respectively. All compounds were injected intraperitoneally to each mouse an hour prior to seizure induced by injection of 60 mg/kg PTZ and observed their behavior for 30 minutes. The result showed that the IV at 75 µmol/kg could delay the latency to first twitch and decrease percent mortality compared to control group.