22 January 2024
GPR88 is a G-protein coupled receptor (GPCR) expressed primarily in the GABAergic medium spiny neurons of the striatum, and to a lesser extent in the cerebral cortex, amygdala, and hypothalamus. Although its exact function and endogenous ligands are unknown, expression studies indicate its possible involvement in processes such as locomotion, learning, emotional reactions, and social interactions, as well as reward and motivation behaviors.
Research into the role of GPR88 has been hampered by the absence of agonists or positive allosteric modulators which can efficiently cross the blood-brain barrier. BI-9508 is a next generation, brain-penetrant molecule lacking the primary amine associated with high P-glycoprotein (PGP) efflux of other GPR88 agonists reported to date. Its good metabolic stability and in vivo profile render it suitable for acute rodent studies.
As part of our commitment to open science, BI-9508 is now available on opnMe free of charge to allow further exploration of GPR88’s role in the context of central nervous system processes. Please note that you retain full ownership and control of your results, which we encourage you to publish.
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About BI-9508:
BI-9508 is a potent, selective and brain-penetrant agonist of GPR88. Its favorable in vivo PK properties render it a useful tool compound to elucidate the intracellular signaling mechanisms and physiological functions of GPR88. BI-0823, a closely related compound lacking an aryl group that is essential for agonist activity, is available as a negative control.
About opnMe:
opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. As part of our first pillar, the “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. These are complemented by “Molecules for Collaboration” where we offer access to unprecedented, often unpublished molecules, together with an attractive funding package. Interested scientists are invited to submit testable research hypotheses with these assets. With our “opn2EXPERTS” program, we enlist advice on key scientific issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs, such as our recent call on “progressing sustainable drug delivery device technologies”.