A series of novel 6-(4-benzylpiperazin-1-yl)benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl]piperazin-1-yl)benzodioxane (2d) had high affinity and selectivity for the D(4) dopamine receptor subtype and was identified as a D(4) antagonist via its attenuation of dopamine-induced GTPgamma(35)S binding at the D(4) receptor.
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http://dx.doi.org/10.1016/s0968-0896(01)00226-7 | DOI Listing |
J Toxicol Sci
January 2025
Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health.
In illicit drug markets, the most recently expanding new synthetic opioid subclass is benzimidazoles, also known as nitazenes, which were originally developed as analgesics in the 1950s. The emergence of this classical, potent drug family has attracted extensive research interest in the field of forensic toxicology; however, information on their psychological and physical dependence is very limited. Herein, we evaluated the rewarding effects of four nitazene analogs using a battery of in vivo experiments, with a positive control drug (isotonitazene).
View Article and Find Full Text PDFEnviron Res
January 2025
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China. Electronic address:
Hygienic insecticides are applied directly to the living environment and are closely related to human life. Dimefluthrin (DIM) is one of the most widely used hygienic insecticides globally. However, with increasing mosquito resistance, both the concentration and duration of DIM usage have risen, prompting public concerns regarding its neurotoxic risks, especially for immunocompromised children.
View Article and Find Full Text PDFJ Neurosci
January 2025
Carleton University, Neuroscience Department, Ottawa, ON, Canada,
Ghrelin enhances feeding by activating the growth hormone secretagogue receptor (GHSR). In the brain, GHSRs are expressed in regions responsible for regulating food motivation including the ventral tegmental area (VTA). Endogenous cannabinoids also promote food seeking behaviors through the cannabinoid receptor 1 type (CB-1Rs) in brain regions including the VTA.
View Article and Find Full Text PDFNeuropharmacology
January 2025
Neurosciences PhD Program, School of Pharmacy, University of Kansas, Lawrence, KS, United States; Department of Pharmacology and Toxicology, School of Pharmacy, University of Kansas, Lawrence, KS, United States. Electronic address:
In humans, grief is characterized by intense sadness, intrusive thoughts of the deceased, and intense longing for reunion with the deceased. Human fMRI studies show hyperactivity in emotional pain and motivational centers of the brain when an individual is reminded of a deceased attachment figure, but the molecular underpinnings of these changes in activity are unknown. Prairie voles (Microtus ochrogaster), which establish lifelong social bonds between breeding pairs, also display distress and motivational shifts during periods of prolonged social loss, providing a model to investigate these behavioral and molecular changes at a mechanistic level.
View Article and Find Full Text PDFNPJ Parkinsons Dis
January 2025
Université de Bordeaux, Institut des Maladies Neurodégénératives, Bordeaux, France.
Parkinson's disease arises from the degeneration of dopaminergic neurons in the substantia nigra pars compacta, leading to motor symptoms such as akinesia, rigidity, and tremor at rest. The non-motor component of Parkinson's disease includes increased neuropathic pain, the prevalence of which is 4 to 5 times higher than the general rate. By studying a mouse model of Parkinson's disease induced by 6-hydroxydopamine, we assessed the impact of dopamine depletion on pain modulation.
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