MC-170073

MC-170073 is a potent and highly selective small molecule antagonist of the serotonin 5-HT7 receptor. It was designed as part of a series of functionalized γ-butyrolactones, achieving strong affinity for 5-HT7 (Ki = 89 nM) and antagonist activity (Kb = 18 nM), with very poor binding to other serotonin receptors. MC-170073 demonstrates high aqueous solubility, moderate metabolic stability, and limited inhibition of CYP3A4, 2C9, and 2D6 enzymes. In preclinical mouse models of acute and chronic colitis, administration of MC-170073 delayed onset and reduced disease severity, with improved histopathology and lower inflammatory cytokines. Investigated routes of administration include intraperitoneal injection and oral gavage, with oral bioavailability of approximately 17%. The compound is not a marketed drug and is characterized primarily in research settings for its potential application in inflammatory bowel disease models[1][3].