The synthesis of several bioisosteric analogs based on the 3-OH-phenoxyethylamine dopamine D2 agonist template (i.e., 3) is described. The benzimidazol-2-ones and benzthioimidazol-2-ones (7-10) and 2-trifluoromethyl-benzimidazole (13) were observed to have excellent affinity for the D2 receptor.
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http://dx.doi.org/10.1016/s0960-894x(99)00434-5 | DOI Listing |
Curr Neuropharmacol
January 2025
Clinic Villa Von Siebenthal, Rome, Italy.
Introduction/objective: Schizophrenia with substance use disorder is a complex clinical condition that may increase treatment resistance. Cannabis use disorder is frequently associated with psychosis and the causal link has still to be defined. Partial D2/3 agonists may ensure limbic dopamine release normalization while avoiding reduced frontocortical dopamine release, which would contribute to negative symptoms.
View Article and Find Full Text PDFSci Rep
January 2025
Physical Sciences Platform, Sunnybrook Research Institute, Toronto, ON, Canada.
Parkinson's disease (PD) is a progressive disorder that affects the nervous system and causes regions of the brain to deteriorate. In this study, we investigated the effects of MR-guided focused ultrasound (MRgFUS) for the delivery of human mesenchymal stem cells (MSCs) on the 6-hydroxydopamine (6-HODA)-induced PD rat model. MRgFUS-induced blood-brain barrier (BBB) permeability modulation was conducted using an acoustic controller with the targets at the striatum (ST) and SN.
View Article and Find Full Text PDFJ Neurol
January 2025
Center for Psychopharmacology, Diakonhjemmet Hospital, Oslo, Norway.
Background: Impaired impulse control is often seen in Parkinson's disease (PD) patients using dopamine agonists.
Methods: We performed a therapeutic drug monitoring study of 100 PD patients using ropinirole or pramipexole extended release. Three blood samples were collected on the same day.
Elife
January 2025
Department of Neurology, University of Iowa, Iowa City, United States.
The role of striatal pathways in cognitive processing is unclear. We studied dorsomedial striatal cognitive processing during interval timing, an elementary cognitive task that requires mice to estimate intervals of several seconds and involves working memory for temporal rules as well as attention to the passage of time. We harnessed optogenetic tagging to record from striatal D2-dopamine receptor-expressing medium spiny neurons (D2-MSNs) in the indirect pathway and from D1-dopamine receptor-expressing MSNs (D1-MSNs) in the direct pathway.
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