Article
Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor.
Nature communications - 14 Feb 2018
Gray David L, Allen John A, Mente Scot, O'Connor Rebecca E, DeMarco George J, Efremov Ivan, Tierney Patrick, Volfson Dmitri, Davoren Jennifer, Guilmette Edward, Salafia Michelle, Kozak Rouba, Ehlers Michael D
Abstract excerpt
Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a therapeutic strategy for neurologic and psychiatric diseases due to the fundamental role of D1Rs in motor function, reward processing, and cognition. All known D1R-selective agonists are catechols, which are rapidly metabolized and desensitize the D1R after prolonged exposure, reducing agonist response. As such, drug-like...
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