| Project/Area Number |
07558223
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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| Allocation Type | Single-year Grants |
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| Section | 試験 |
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| Research Field |
Functional biochemistry
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| Research Institution | KYOTO UNIVERSITY |
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Principal Investigator |
NAKANISHI Shigetada Kyoto University, Medicine, Professor, 医学研究科, 教授 (20089105)
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| Project Period (FY) |
1995 – 1996
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| Project Status |
Completed (Fiscal Year 1996)
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| Budget Amount *help |
¥3,600,000 (Direct Cost: ¥3,600,000)
Fiscal Year 1996: ¥3,600,000 (Direct Cost: ¥3,600,000)
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| Keywords | metabotropic glutamate receptor1 / agonist・antagonist / receptor-expressing cell / phenylglycine derivative / AMPA derivative / structure-activity relationship17GA01 : N.Sekiyama, et al. / アゴニスト / アンタゴニスト / アンダゴニスト |
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| Research Abstract |
The metabotropic glutamate receptors (mGluRs) consist of 8 different subtypes. The aim of this research is to develop new agonists and antagonists of defferent mGluR subtypes by examining the agonistic and antagonistic effects of a large number of phenylglycine derivatives and other compounds on the signal transduction of representative mGluR1, mGluR2 and mGluR4/mGluR6 subtypes expressed in CHO cells. We have succeeded in developing new agonists and antagonists and have elucidated structure-activity relationships of these compounds for different mGluR subtypes.
1.Our study of phenylglycine derivatives indicates that the nature and positions of side chains and ring substituents incorporated into the phenylglycine structure are critical in determining the agonist and antagonist activities of this group of compounds on different mGluR subtypes.
2.alpha-Methylation produces different effects, depending on the chemical structures of lead compounds and on the subtype of mGluR tested.
3.We have also demonstrated that new glutamate analogues such as 2-amino-4 (3-hydroxy-5-methylisoxazol-4-yl) butyric acid have agonist activities on mGluRs.
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