Fenobam 是可口服的、可穿过血脑屏障的mGluR5拮抗剂，具有抗焦虑活性，在大鼠和人重组 mGlu5 受体上的Kd值分别 54 和 31 nM。它有反向激动剂活性，可阻断 mGlu5 受体活性，IC50为 84 nM。

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

Fenobam sulfate (30-60 mg/kg; p.o.) inhibited cocaine self-administration significantly [3].

57653-26-6

C11H11ClN4O2

266.68

DMSO:55 mg/ml (206.24 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years