异恶唑探索谷氨酸受体-猫眼课题宝

异恶唑探索谷氨酸受体

批准号：

6471158

负责人：

Nicholas R. Natale

金额：

$14.85万

依托单位：

UNIVERSITY OF IDAHO

依托单位国家：

美国

项目类别：

财政年份：

1999

资助国家：

美国

项目状态：

已结题

起止时间：

1999-05-01 至 2005-12-31

来源：

https://reporter.nih.gov/project-details/6471158

关键词：

AMPA receptors aminoacid analog anticonvulsants chemical models chemical structure function chemical synthesis conformation drug screening /evaluation excitatory aminoacid fluorescent dye /probe glutamate receptor high performance liquid chromatography isoxazoles neurotransmitter agonist neurotransmitter antagonist protein isoforms receptor binding receptor expression stereochemistry

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英文摘要

DESCRIPTION: (provided by applicant) Glutamate receptors are important in the transmision of signals across the synapses between nerve cells. Isoxazoles such as Amino-Methyl-Isoxazole Propionic Acid (AMPA) have been found to be useful in the characterization of Glutamate receptor subtypes. We have obtained results in the first granting period which show promise for the efficient preparation of chiral isoxazole glutamate receptor ligands. In the current granting period we propose (1) to complete the synthesis of a defined set of C(5) functionalized AMPA analogues based on structure based design using the G1uR2 subtype binding domain, (2) prepare linked antagonists and agonists to probe the Gouaux Glutamate receptor Activation and Antagonism model and (3) prepare glutamate receptor ligands covalently linked to molecular probes to help elucidate the conformation dynamics of the intact membrane bound receptor during activation and modulation.

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