Development of anti-parkinsonian drug using structure-activity relationship
Development of anti-parkinsonian drug using structure-activity relationship
批准号:
14370757
负责人:
OHTA Shigeru
金额:
$8.26万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (B)
财政年份:
2002
资助国家:
日本
项目状态:
已结题
起止时间:
2002 至 2003
中文摘要
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英文摘要
The purpose of this project is to elucidate an anti-parkinsonian drug. Our group has found that 1 MeTIQ is a very good candidate for the anti-parkinsonian drug. We studied the structure activity relationship for 1MeTIQ derivatives using inhibition of dopaminergic cell toxicity. As the results, 1-benzyl DIQ, an oxidative metabolite of 1-benzyl TIQ, has strong cell toxicity. So the matabolism is very important factor. 7-OH-1MeTIQ has the most potent anti-parkinsonian drug. So it is very suitable candidate for Parkinson's disease.
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K.Okuda, Y.Kotake, S.Ohta: "Determination method of 1-methyl-1,2,3,4-tetrahydroisoquinoline, an endogenous parkinsonism-preventing substance, by radioimmunoassay."Life Sci.. 70. 2871-2883 (2002)
K.Okuda、Y.Kotake、S.Ohta:“通过放射免疫测定法测定内源性帕金森病预防物质 1-甲基-1,2,3,4-四氢异喹啉。”Life Sci.. 70. 2871-2883
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作者:
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通讯作者:
A.Storch, et al.: "Selective dopaminergic neurotoxicity of isoquinoline derivatives related to Parkinson's disease : studies using heterologous expression systems of the dopamine transporter."Biochem.Pharmacol.. 63. 909-920 (2002)
A.Storch 等人:“与帕金森病相关的异喹啉衍生物的选择性多巴胺能神经毒性:使用多巴胺转运蛋白异源表达系统的研究。”Biochem.Pharmacol.. 63. 909-920 (2002)
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通讯作者:
K.Okuda, et al.: "Neuroprotective or neurotoxic activity of 1-methyl 1,2,3,4-tetra-hydroisoquinoline and related compounds"Bioorg. Med. Chem. Lett.. 13. 2853-2855 (2003)
K.Okuda 等人:“1-甲基 1,2,3,4-四氢异喹啉及相关化合物的神经保护或神经毒性活性”Bioorg。
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通讯作者:
Y.Kotake: "Neurotoxicity of an endogenous brain amine, 1-benzyl-1,2,3,4-tetrahydroisoquinoline, in organotypic slice co-culture of mesencephalon and striatum"Neuroscience. 117. 63-70 (2003)
Y.Kotake:“内源性脑胺 1-苄基-1,2,3,4-四氢异喹啉在中脑和纹状体的器官切片共培养中的神经毒性”神经科学。
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发表时间:
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作者:
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通讯作者:
K.Okuda, Y.Kotake, S.Ohta.: "Neuroprotective or neurotoxic activity of 1-methyl 1,2,3,4-tetra-hydroisoquinoline and related compounds."Bioorg.Med.Chem.Lett.. 13. 2853-2855 (2003)
K.Okuda、Y.Kotake、S.Ohta.:“1-甲基 1,2,3,4-四氢异喹啉及相关化合物的神经保护或神经毒性活性。”Bioorg.Med.Chem.Lett.. 13. 2853
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共 14 条
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Drug development using novel animal model based on the pathogenesis of Parkinson' s disease-related disorders
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Parkinsonism-inducing mechanism by endogenous multifunctional neurotoxins in the brain
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Early markers of Parkinson's disease
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