Aims: To evaluate the antidepressant-like effect of compound GW117 in rodents using in vitro binding and uptake assays as well in vivo behavioral tests.

Methods: We investigated the target profile of GW117 using [ S]-GTPγS and [ H]PIP binding. Using the forced swimming test and chronic unpredictable stress in rats, tail suspension test in mice and rats, and learned helplessness model in mice, we further revealed the antidepressant-like and anxiolytic-like effects of GW117.

Results: The current study suggests that GW117 displays serotonin 2C (5-HT ) receptor antagonist and melatonin type 1 and 2 (MT /MT ) receptor agonist properties, as well as evident antidepressant and anxiolytic effects.

Conclusion: These data suggest that GW117 is probably a potent antidepressant.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8111499PMC
http://dx.doi.org/10.1111/cns.13630DOI Listing

Publication Analysis

Top Keywords

serotonin 5-ht
8
5-ht receptor
8
receptor antagonist
8
antagonist melatonin
8
/mt receptor
8
receptor agonist
8
gw117
5
gw117 novel
4
novel serotonin
4
receptor
4

Similar Publications

Brain serotonin dysregulation is associated with dementia and neuropsychiatric symptomology. However, the prognostic utility of circulating serotonin levels in detecting features of prodromal dementia including functional decline, cognitive impairment, mild behavioural impairment and brain atrophy remains unclear. In this prospective study of memory clinic subjects followed-up for ≤5 years, dementia-free subjects, classified as having no cognitive impairment or cognitive impairment, no dementia at baseline, underwent annual neuropsychological assessments including Montreal Cognitive Assessment, Global Cognition scores and Clinical Dementia Rating Scale Global Scores (where a ≥ 0.

View Article and Find Full Text PDF

The coexistence of depression and type 2 diabetes mellitus (T2DM) can significantly worsen disease prognosis and lower quality of life. Emerging evidence suggests that vitamin D deficiency contributes to the progression of T2DM and is closely associated with the development of depression. The aim of this study was to investigate the effects of cholecalciferol on depression in patients with T2DM, exploring its mechanisms by analyzing its impact on C-peptide, serotonin, and neurotrophin-3 levels.

View Article and Find Full Text PDF

Patent review of novel compounds targeting opioid use disorder (2018-2024).

Expert Opin Ther Pat

January 2025

Department of Pharmaceutical and Biomedical Sciences, Rudolph H. Raabe College of Pharmacy, Ohio Northern University, Ada, OH, USA.

Introduction: Opioids have served as a cornerstone in pain management for decades. However, the emergence of increasingly potent synthetic analogs brings forth a range of side effects, including respiratory depression, tolerance, dependence, constipation, and, more importantly, the development of severe and debilitating opioid use disorder (OUD). Search for therapeutics to mitigate OUD has been challenging and this has called for novel approaches that include design of small molecules targeting neuronal circuits involved in addiction (opioid, dopamine, serotonin, norepinephrine, and glutamate receptors, etc.

View Article and Find Full Text PDF

Acute stress disorder (ASD) is a transient psychiatric disorder that may arise subsequent to abrupt, extreme trauma exposure, and serves as a reliable indicator for the subsequent development of posttraumatic stress disorder (PTSD) (Bryant, 2011; Battle, 2013). It exhibits rapid progression in the aftermath of trauma and persists for a duration of days or weeks (not exceeding one month), manifesting symptoms of dissociation, re-experiencing, avoidance, and hyperarousal (Bielas et al., 2018).

View Article and Find Full Text PDF

3,4-methylenedioxymethamphetamine (MDMA; commonly referred to as "ecstasy" or "molly") is a substituted amphetamine drug that is used recreationally for its acute psychoactive effects, including euphoria and increased energy, as well as prosocial effects such as increased empathy and feelings of closeness with others. Acute adverse effects can include hyperthermia, dehydration, bruxism, and diaphoresis. Post-intoxication phenomena may include insomnia, anhedonia, anxiety, depression, and memory impairment, which can persist for days following drug cessation.

View Article and Find Full Text PDF

Want 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!