mGlu4受体变构调节剂PHCCC对大鼠的抗焦虑样作用。
Anxiolytic-like effects of PHCCC, an allosteric modulator of mGlu4 receptors, in rats.
作者信息
Stachowicz Katarzyna, Kłak Kinga, Kłodzińska Aleksandra, Chojnacka-Wojcik Ewa, Pilc Andrzej
机构信息
Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31-343 Krakow, Poland.
出版信息
Eur J Pharmacol. 2004 Sep 13;498(1-3):153-6. doi: 10.1016/j.ejphar.2004.07.001.
We examined the potential anxiolytic-like activity of (-)-N-phenyl-7-(hydroxyimino) cyclopropa[b]chromen-1a-carboxamide (PHCCC), an allosteric modulator of metabotropic glutamate4 receptors (mGlu4), after administration into the basolateral amygdala, using the conflict drinking Vogel test in rats as a model. The results indicate that PHCCC, but not 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester (CPCCOEt), the selective antagonist of group mGlu1 receptors, showed significant, dose-dependent anticonflict effects without affecting the threshold current or water intake. The results indicate that positive allosteric modulation of mGlu4 receptors may be a useful therapeutic approach to anxiety.
我们使用大鼠冲突饮水Vogel试验作为模型，研究了代谢型谷氨酸受体4（mGlu4）的变构调节剂（-）-N-苯基-7-（羟基亚氨基）环丙[b]色烯-1a-甲酰胺（PHCCC）注入基底外侧杏仁核后的潜在抗焦虑样活性。结果表明，PHCCC显示出显著的、剂量依赖性的抗冲突效应，且不影响阈电流或饮水量，但代谢型谷氨酸受体1组的选择性拮抗剂7-（羟基亚氨基）环丙[b]色烯-1a-羧酸乙酯（CPCCOEt）则无此效应。结果表明，对mGlu4受体的正向变构调节可能是一种治疗焦虑症的有效方法。
Zotero 插件