Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor

Dopamine receptor agonists are used for the treatment of various psychiatric diseases. Here, the authors screen approximately three million compounds and identify a novel class of D1R agonists that do not have a catechol scaffold and possess promising pharmacokinetic properties.

Saved in:
Bibliographic Details
Main Authors: David L. Gray, John A. Allen, Scot Mente, Rebecca E. O’Connor, George J. DeMarco, Ivan Efremov, Patrick Tierney, Dmitri Volfson, Jennifer Davoren, Edward Guilmette, Michelle Salafia, Rouba Kozak, Michael D. Ehlers
Format: article
Language:EN
Published: Nature Portfolio 2018
Subjects:
Q
Online Access:https://doaj.org/article/8a74eb3e0a2d4c1fa0ce2b3e319fdc9f
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Dopamine receptor agonists are used for the treatment of various psychiatric diseases. Here, the authors screen approximately three million compounds and identify a novel class of D1R agonists that do not have a catechol scaffold and possess promising pharmacokinetic properties.