compound introduction
Fenobam 是一种选择性、口服活性的、穿过血脑屏障的 mGluR5 拮抗剂，其作用于变构调节位点 (在大鼠和人重组 mGlu5 受体上的 Kd 值分别 54 nM 和 31 nM)。Fenobam 具有反向激动剂活性，其阻断 mGlu5 受体活性，IC50为 84 nM。 Fenobam 具有抗焦虑活性。 Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity。
