CGP55845 is a potent and selective antagonist of the GABAB receptor, effectively blocking agonist binding. With an IC50 value of 5 nM, it demonstrates significant inhibition of GABA and glutamate release. The compound exhibits a high affinity for the GABAB receptor, with an apparent Kd of 30 nM. CGP55845 is comparable in potency to 100 μM CGP 35348 for reversing the inhibitory effects of (R)-(-)-baclofen, making it a valuable tool for research into GABAergic signaling and related physiological functions.
CGP55845 is a potent and selective antagonist of the GABAB receptor, effectively blocking agonist binding. With an IC50 value of 5 nM, it demonstrates significant inhibition of GABA and glutamate release. The compound exhibits a high affinity for the GABAB receptor, with an apparent Kd of 30 nM. CGP55845 is comparable in potency to 100 μM CGP 35348 for reversing the inhibitory effects of (R)-(-)-baclofen, making it a valuable tool for research into GABAergic signaling and related physiological functions.
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