A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics. The title compounds were synthesized and tested for blockade of [3H]YM-09151 binding in cloned African green monkey dopamine D2 receptor preparations. The binding affinity data thus obtained were compared against that of the benzamides and a previously described series of 2-phenyl-5-(aminomethyl)-pyrroles.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm00012a026 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mu opioid receptors expressed in striatal D2 medium spiny neurons have divergent contributions to cocaine and morphine reward.
Neuroscience
January 2025
Institute for Neuroscience, The University of Texas at Austin, Austin, TX, USA; Waggoner Center for Alcohol & Addiction Research, The University of Texas at Austin, Austin, TX, USA; Department of Neuroscience, The University of Texas at Austin, Austin, TX, USA; Department of Neurology, Dell Medical School, The University of Texas at Austin, Austin, TX, USA. Electronic address:
While our understanding of the neurobiological mechanisms underlying cocaine and opiate reward has historically been dopamine-focused, evidence from genetic and pharmacological approaches indicates that µ-opioid receptors (MORs) in the striatum are important contributors. Within the striatum, MORs are expressed in both dopamine D1-receptor and D2-receptor expressing GABAergic medium spiny neurons (MSNs), as well as in interneurons and various afferents. Thus, it remains unclear how these distinct MOR populations regulate drug reward.
View Article and Find Full Text PDFD dopamine / mu opioid receptor interactions in operant conditioning assays of pain-depressed responding and drug-induced rate suppression, and a conditioned place preference procedure: assessment of therapeutic index in male Sprague Dawley rats.
Psychopharmacology (Berl)
January 2025
Department of Psychology, University of New England, Biddeford, ME, USA.
Rationale And Objectives: In vivo receptor interactions vary as a function of behavioral endpoint, with key differences between reflexive and non-reflexive measures that assess the motivational aspects of pain and pain relief. There have been no assessments of D dopamine agonist / mu opioid receptor (MOR) agonist interactions in non-reflexive behavioral measures of pain. We examined the hypothesis that D/MOR mixtures show enhanced effectiveness in blocking pain depressed behaviors while showing decreased side effects such as sedation and drug reward.
View Article and Find Full Text PDFIn the later stages of Parkinson's disease (PD), patients often manifest levodopa-induced dyskinesia (LID), compromising their quality of life. The pathophysiology underlying LID is poorly understood, and treatment options are limited. To move toward filling this treatment gap, the intrinsic and synaptic changes in striatal spiny projection neurons (SPNs) triggered by the sustained elevation of dopamine (DA) during dyskinesia were characterized using electrophysiological, pharmacological, molecular and behavioral approaches.
View Article and Find Full Text PDFInhibition of mPFC norepinephrine improved chronic post-thoracotomy pain in adult rats.
Ann Med
December 2025
Department of Anesthesiology, The Third Xiangya Hospital, Central South University, Changsha, Hunan Province, China.
Background: Chronic post-thoracotomy pain (CPTP) is characterized by high incidence, long duration, and severity of pain. Medial prefrontal cortex (mPFC) is a brain region closely associated with chronic pain, and norepinephrine is involved in pain regulation. But the role of mPFC norepinephrine in CPTP and its possible mechanism is unclear.
View Article and Find Full Text PDFNeurotransmitter and metabolic effects of interferon-alpha in association with decreased striatal dopamine in a Non-Human primate model of Cytokine-Induced depression.
Brain Behav Immun
January 2025
Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, Atlanta, GA 30322, USA; Winship Cancer Institute, Emory University, Atlanta, GA 30322, USA. Electronic address:
Inflammatory stimuli administered to humans and laboratory animals affect mesolimbic and nigrostriatal dopaminergic pathways in association with impaired motivation and motor activity. Alterations in dopaminergic corticostriatal reward and motor circuits have also been observed in depressed patients with increased peripheral inflammatory markers. The effects of peripheral inflammation on dopaminergic pathways and associated neurobiologic mechanisms and consequences have been difficult to measure in patients.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!