CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen.
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