Drug intelligence / Profile preview

DPI-221

Development stage
Preclinical
Lead developer
Enhance Biotech
Modality
Small Molecules
Administration
Oral
01

Overview

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].

Other names
4-((alpha-S)-alpha-((2S,5R)-2,5-dimethyl-4-(3-fluorobenzyl)-1-piperazinyl)benzyl)-N,N-diethylbenzamideN,N-diethyl-4-((S)-((2S,5R)-4-((3-fluorophenyl)methyl)-2,5-dimethyl-1-piperazinyl)phenylmethyl)benzamide519058-15-2UNII-X9LJN69TFKUNII-X-9LJN69TFKUNII-X 9LJN69TFKX9LJN69TFKX-9LJN69TFKX 9LJN69TFK
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)

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