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UD-030 is a novel, highly selective, nonpeptide small molecule antagonist of the mu-opioid receptor (MOP). It exhibits high binding affinity for the human MOP (Ki = 3.1 nM) and demonstrates over 100-fold selectivity over delta-opioid, kappa-opioid, and nociceptin receptors. In preclinical studies, oral administration of UD-030 dose-dependently suppressed the acquisition and expression of morphine-induced conditioned place preference (CPP) in mice, with efficacy comparable to naltrexone. Its high selectivity for the MOP suggests it may offer a therapeutic advantage for the treatment of opioid use disorder by specifically blocking opioid-mediated reward pathways with reduced off-target activity compared to traditional, less selective antagonists.
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