Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
作者:
主题词
1-甲基-4-苯基-1,2,3,6-四氢吡啶(1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine);投药, 口服(Administration, Oral);别构调节(Allosteric Regulation);动物(Animals);抗震颤麻痹药(Antiparkinson Agents);生物利用度(Biological Availability);细胞膜通透性(Cell Membrane Permeability);狗(Dogs);运动障碍, 药物性(Dyskinesia, Drug-Induced);HEK293细胞(HEK293 Cells);人类(Humans);超敏反应, 迟发型(Hypersensitivity, Delayed);左旋多巴(Levodopa);成束猴(Macaca fascicularis);男(雄)性(Male);微粒体, 肝(Microsomes, Liver);模型, 分子(Models, Molecular);帕金森病(Parkinson Disease);吡嗪类(Pyrazines);吡唑类(Pyrazoles);放射配体测定(Radioligand Assay);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);构效关系(Structure-Activity Relationship)
DOI
10.1021/jm401622k
PMID
24392688
发布时间
2014-02-13
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