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DPI-221 is an investigational small molecule that acts as a **selective delta-opioid receptor agonist** with high affinity for the delta receptor and much lower affinity for the mu and kappa opioid receptors. It has been studied primarily for its effects on **bladder function**, where it significantly increases the interval between micturition events in animal models without substantially reducing voiding pressure. The mechanism of action is via delta-opioid receptor activation, demonstrated by pharmacological blockade of its effects with the delta-selective antagonist naltrindole. Importantly, DPI-221 shows a favorable preclinical safety profile compared to other delta agonists, with very low incidence of seizure-like convulsions when administered orally. It is not currently approved for clinical use and remains at the experimental stage[1][3][5].
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