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triazole 187
- Development stage
- Preclinical
- Modality
- Small Molecules
01
Overview
triazole 187 is a potent, G protein signaling-biased kappa-type opioid receptor (KOR) agonist developed by researchers at the University of North Carolina at Chapel Hill and the University of Florida (specifically UF Scripps Biomedical Research). Unlike conventional KOR agonists such as U50,488H, which cause significant sedation, dysphoria, and diuresis, triazole 187 preferentially activates G protein-mediated signaling over beta-arrestin2 recruitment. In preclinical mouse models, triazole 187 demonstrates robust antipruritic efficacy and produces anxiolytic-like behaviors without inducing sedation or severe diuresis, making it a promising candidate for the treatment of chronic itch, pain, and anxiety disorders.
- Other names
- Triazole 187Triazole187Triazole-187
02
Targets
KOR (Kappa opioid receptor)
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