PAC-832

PAC-832 is a selective, brain-penetrant small-molecule galanin receptor 1 (GalR1) antagonist being developed for the treatment of Alzheimer's disease. Developed by Pace Pharmaceuticals, the compound exhibits sub-micromolar potency (IC50 = 0.28 μM) and greater than 30-fold selectivity over GalR2 and GalR3. By selectively blocking GalR1, PAC-832 aims to reverse galanin-mediated suppression of acetylcholine release in the brain, thereby improving cognitive function. In preclinical mouse models of cholinergic dysfunction, systemic administration of PAC-832 demonstrated high brain exposure and significantly improved spatial working memory and recognition memory. The drug is currently undergoing IND-enabling studies in preparation for Phase 1 clinical trials.