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June 19, 2026JACS AuOpen Access

A Ligand-Triggered Receptor Conformation Enables the Design of Selective Agonists for the Dopamine 3 Receptor (D 3 R) Using a Bitopic Strategy

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Authors

SASandra Arroyo‐UreaANAntonina L. NazarovaAKAlexander Knieb

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Overview

Randomized trial demonstrates the design of selective agonists for dopamine 3 receptor, suggesting novel approaches for neurotherapeutics.

Key Points

  • The aim is to design selective agonists for the dopamine 3 receptor using a ligand-triggered conformation.
  • Utilized rational bitopic drug design based on ligand-induced receptor conformation.
  • Synthesized and characterized D 3 R agonists with varying selectivity and potency.
  • Focused on the first transmembrane helix of the dopamine receptors to enhance selectivity.
  • Developed D 3 R partial agonists with >575,000- and >750,000-fold subtype selectivity.
  • Reported full agonists exhibiting >2,800- and 6,300-fold selectivity for D 3 R.
  • Achieved picomolar potencies and significant efficacy with newly designed compounds.

Cite This Study

Arroyo‐Urea et al. (2026) studied this question.

synapsesocial.com/papers/6a34df7565a5b0777af2e8eahttps://doi.org/10.1021/jacsau.6c00654
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Also Consider

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