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PZM21

Development stage
Preclinical
Lead developer
Epiodyne
Modality
Small Molecules
Administration
Not Established; Used Experimentally In Preclinical Research (typically Parenteral Routes In Animal Studies)[6]
01

Overview

PZM21 is an experimental small molecule opioid analgesic that acts as a potent and selective agonist of the μ-opioid receptor. It was designed using structure-based virtual screening to bias signaling toward G protein activation over β-arrestin 2 recruitment. This "G protein-biased" profile was initially reported to provide effective analgesia with reduced side effects such as respiratory depression and constipation compared to classical opioids like morphine. However, subsequent studies have shown that at higher doses, PZM21 can still produce typical opioid side effects including respiratory depression and tolerance. The compound has been primarily studied in preclinical models for pain management[1][3][5][6].

Other names
(S,S)-1-[2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-(1-thiophen-3-ylpropan-2-yl)urea
02

Targets

MOR (Mu opioid receptor)

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