2,3-二氢-6,7-二氯吡啶并[2,3-b]吡嗪-8-氧化物作为具有体内活性的选择性甘氨酸拮抗剂。
2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity.
作者信息
Micheli F, Cugola A, Donati D, Missio A, Pecunioso A, Reggiani A, Tarzia G
机构信息
GlaxoWellcome S.p.A., Medicines Research Center, Verona, Italy.
出版信息
Bioorg Med Chem. 1997 Dec;5(12):2129-32. doi: 10.1016/s0968-0896(97)00156-9.
PMID:9459010
Abstract
2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the effectiveness of glycine antagonists in vivo.
摘要
合成了2,3 - 二氢 - 6,7 - 二氯 - 吡啶并[2,3 - b]吡嗪 - 8 - 氧化物，并对其在NMDA受体上士的宁不敏感甘氨酸结合位点的体外/体内拮抗活性进行了评估，结果表明它是评估甘氨酸拮抗剂体内有效性的有用工具。
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