CGP36216 hydrochloride acts as a selective antagonist at the presynaptic GABA receptor, specifically binding to the GABAB receptor with a Ki value of 0.3 μM. This compound is leveraged in research focused on anxiety and trauma-related disorders [1] [2].

CGP36216 对 GABA 的突触后受体无效，然而在突触前受体表现出较高的活性。CGP36216（100 µM）能够提高 VTA-DA 神经元自发放电频率。