alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.

alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.
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α-取代的使君子酸类似物:新型代谢型谷氨酸受体 II 组选择性拮抗剂。

DOI:
10.1016/s0960-894x(98)00052-3
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发表时间:
1998
影响因子:
2.7
通讯作者:
Wroblewski,JT
Wroblewski,JT
中科院分区:
医学4区
文献类型:
--
作者:
Kozikowski,AP;Steensma,D;Varasi,M;Pshenichkin,S;Surina,E;Wroblewski,JT

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Syntheses of both the α-methyl and benzyl analogs of quisqualic acid are described. Testing of these compounds for their activity at excitatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results in the loss of quisqualate's potent agonist action at both non-NMDA ionotropic glutamate receptors as well as at group I mGluRs, while allowing these analogs to acquire antagonist properties with relative selectivity for group II metabotropic glutamate receptors.