The mGlu4 receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide acts as a direct agonist at mGlu6 receptors
The mGlu4 receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide acts as a direct agonist at mGlu6 receptors
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DOI：
10.1016/j.ejphar.2008.06.054
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发表时间：
2008-07-28
影响因子：
5
通讯作者：
Kammermeier, Paul J.
中科院分区：
文献类型：
--
作者：
Beqollari, Donald;Kammermeier, Paul J.
研究了MGlu(4)受体变构调节剂n-苯基-7-（羟亚胺）环丙酚-lacarboxamide （PHCCC）对密切相关的MGlu(6)受体的影响。通过表达mGlu(4)和mGlu(6)受体对大鼠颈上神经节离体交感神经元钙电流的调节来测定受体活性。有和没有PHCCC的谷氨酸浓度-反应曲线证实该药物是mGlu(4)受体的变构调节剂，没有直接的激动剂活性。相反，PHCCC直接激活mGlu(6)受体，而不增强谷氨酸的活性。因此，PHCCC是一种直接的mGlu(6)受体激动剂，但缺乏变构调节特性。(C) 2008 Elsevier B.V.版权所有
Effects of the MGlu(4) receptor allosteric modulator N-phenyl-7-(hydroxyimino)cyclopropalblchromen-lacarboxamide (PHCCC) were tested on closely related mGlu(6) receptors. Modulation of native calcium currents in isolated sympathetic neurons from rat superior cervical ganglion by expressed mGlu(4) and mGlu(6) receptor was used to assay receptor activity. Glutamate concentration-response curves with and without PHCCC confirmed that the drug is an allosteric modulator of mGlu(4) receptor, without direct agonist activity. Conversely, PHCCC directly activates the mGlu(6) receptor and does not enhance activity of glutamate. Therefore, PHCCC is a direct mGlu(6) receptor agonist, but lacks allosteric modulatory properties. (C) 2008 Elsevier B.V. All rights reserved.