CGP55845

CGP55845 is a synthetic pharmacological tool used primarily in neuroscience research as a selective antagonist of the GABA-B receptor. By binding to the GABA-B receptor, it blocks the action of the endogenous neurotransmitter GABA and prevents GABA-B–mediated signaling, allowing researchers to dissect the role of GABA-B receptors in various physiological processes. The compound exhibits high selectivity for GABA-B receptors relative to other GABA receptor subtypes, making it useful for isolating GABA-B–dependent effects in experimental systems.

GABA-B receptors are G protein–coupled receptors that function as heterodimers composed of GABA-B1 and GABA-B2 subunits. Antagonists like CGP55845 inhibit receptor activity, which can influence both presynaptic and postsynaptic inhibitory mechanisms. As a research tool, CGP55845 is employed in in vitro preparations such as brain slices and cultured neurons, as well as in in vivo studies in rodents, to investigate the involvement of GABA-B signaling in processes including analgesia, motor control, learning and memory, and seizure susceptibility.

CGP55845 is typically used to characterize the contribution of GABA-B receptor activity in various pharmacological and physiological experiments. Like other research chemicals, its use requires appropriate laboratory safety measures and ethical considerations. It is one of several CGP-series compounds developed to enable selective dissection of GABA-B receptor function and to aid in the interpretation of GABA-B–related phenomena in the nervous system.