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Development of kainic acid analogs a...

Shou, Xiaohong.

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Development of kainic acid analogs as ionotropic glutamate receptor ligands.

紀錄類型:	書目-電子資源 : Monograph/item
正題名/作者:	Development of kainic acid analogs as ionotropic glutamate receptor ligands./
作者:	Shou, Xiaohong.
面頁冊數:	251 p.
附註:	Source: Dissertation Abstracts International, Volume: 66-05, Section: B, page: 2593.
Contained By:	Dissertation Abstracts International66-05B.
標題:	Chemistry, Organic. -
電子資源:	http://pqdd.sinica.edu.tw/twdaoapp/servlet/advanced?query=3175301
ISBN:	9780542136122

Development of kainic acid analogs as ionotropic glutamate receptor ligands.
Shou, Xiaohong.

Development of kainic acid analogs as ionotropic glutamate receptor ligands. - 251 p.

Source: Dissertation Abstracts International, Volume: 66-05, Section: B, page: 2593.

Thesis (Ph.D.)--University of California, Irvine, 2005.

Ionotropic glutamate receptors (iGluRs) play an essential role in mediating excitatory neurotransmission in the central nervous system, but studies of the physiological function of the iGluRs have been hampered by the lack of subtype-selective ligands. The development of specific ligands for the iGluR subtypes is not only essential to gain a deeper understanding of these receptors, but also to facilitate the discovery of therapeutically useful drugs to treat neurological disorders.

ISBN: 9780542136122Subjects--Topical Terms:

516206
Chemistry, Organic.

Development of kainic acid analogs as ionotropic glutamate receptor ligands.
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245 1 0 $a Development of kainic acid analogs as ionotropic glutamate receptor ligands.
300 $a 251 p.
500 $a Source: Dissertation Abstracts International, Volume: 66-05, Section: B, page: 2593.
500 $a Chair: A. Richard Chamberlin.
502 $a Thesis (Ph.D.)--University of California, Irvine, 2005.
520 $a Ionotropic glutamate receptors (iGluRs) play an essential role in mediating excitatory neurotransmission in the central nervous system, but studies of the physiological function of the iGluRs have been hampered by the lack of subtype-selective ligands. The development of specific ligands for the iGluR subtypes is not only essential to gain a deeper understanding of these receptors, but also to facilitate the discovery of therapeutically useful drugs to treat neurological disorders.
520 $a Conformationally constrained, indole/indoline analogs based on the well-known iGluR agonist kainic acid were designed and synthesized. Screening for iGluR activity revealed that these compounds are kainate receptor antagonists. The identified pharmacophore, a substituted indole structure, serves as a valuable lead template for the synthesis of a library of subtype selective iGluR ligands. Homology modeling and structure-based design guided the parallel synthesis of 44 such ligands, and two other similar types of iGluR ligands, hexahydroindolines and dihydroisoquinolines, with the greater basicity of the amino group, were synthesized in 4--7 steps.
520 $a In addition, a large-scale synthesis of kainic acid was investigated following a published strategy, and several reactions in this reported synthesis required substantial optimization to improve the yield and ee of the key transformation, an asymmetric ene cyclization, and reduce the overall 7-step synthesis by two steps.
520 $a Finally, interactions of the photo-probe diazokainic acid (DZKA) with the iGluRs were carefully studied in the GluR2, GluR5, and GluR6 subtypes using molecular modeling. The selectivity of photo-active DZKA for KARs was found to be influenced by the distance of the nearby receptor residue side-chains. The hypothesis lays the ground work for the design of selective photo-probes for other receptor subtypes.
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