Blockade of Serotonin 2C Receptors with SB-242084 Moderates Reduced Locomotor Activity and Rearing by Cannabinoid 1 Receptor Antagonist AM-251

Bogáthy, Emese; Kostyalik, Diána; Petschner, Péter; Vas, Szilvia; Bagdy, György

doi:10.1159/000495939

Cited by 7 publications

(4 citation statements)

References 38 publications

(55 reference statements)

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“…The distance travelled by mice from all tested groups was comparable to the one covered by the vehicle-treated animals. Though altered motility of rodents can be expected after administration of cannabinoids [24,25], our outcomes were in line with results published by Kruk-Słomka and colleagues [10].…”

Section: Discussionsupporting

confidence: 92%

Influence of the endocannabinoid system on the antidepressant activity of bupropion and moclobemide in the behavioural tests in mice

et al. 2020

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Background Though there are several classes of antidepressant drugs available on the pharmaceutical market, depression that affects globally over 320 million people is still undertreated. Scientists have made attempts to develop novel therapeutical strategies to maximize effectiveness of therapy and minimize undesired reactions. One of the ideas is use of either dual-action agents or combined administration of two substances that affect diverse neurotransmissions. Thus, we investigated whether the selected CB receptor ligands (oleamide, AM251, JWH133, and AM630) can have an impact on the activity of bupropion and moclobemide. Bupropion belongs to the dual acting drugs, whereas moclobemide is an inhibitor of monoamine oxidase. Methods The mice forced swim test and the tail suspension test were applied in order to determine the potential antidepressant-like activity, whereas the HPLC method was used in order to assess the brain concentrations of the tested antidepressants. Results An intraperitoneal injection of sub-effective doses of oleamide (5 mg/kg), AM251 (0.25 mg/kg), and AM630 (0.25 mg/kg) increased activity of bupropion (10 mg/kg) in both behavioural tests. Effects of moclobemide (1.5 mg/kg) were potentiated only by AM251. These results were not influenced by the hypo-or hyperlocomotion of animals. Conclusion The outcomes of the present study revealed that particularly activation or inhibition of the CB 1 receptor function may augment the antidepressant activity of bupropion, whereas only inhibition of the CB 1 receptor function manages to increase activity of moclobemide. Most probably, an interplay between CB receptor ligands and bupropion or moclobemide takes place at the cellular level.

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Section: Discussionsupporting

confidence: 92%

Influence of the endocannabinoid system on the antidepressant activity of bupropion and moclobemide in the behavioural tests in mice

et al. 2020

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“…As mentioned above the inverse agonist Rimonabant, found to be effective for weight-loss and smoking cessation, was quickly withdrawn following the emergence of severe psychiatric side effects. 182 In line with this, CB1 inverse agonist, AM251 has been found to reduce social interactions in rodents 183,184 and nonhuman primates. 115 Interestingly and in contrast to CB1 inverse agonists, two preclinical studies found that administration of a CB1 neutral antagonist, AM4113, did not produce anxiogenic or depressive side effects when administered in rats.…”

Section: Summary Of Current Drugs Targeting the Endocannabinoid Systemmentioning

confidence: 62%

The endocannabinoid system in social anxiety disorder: from pathophysiology to novel therapeutics

Ahmed

Boileau

Foll

et al. 2022

Braz. J. Psychiatry

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Social anxiety disorder (SAD) is a highly prevalent psychiatric disorder that presents with an early age of onset, chronic disease course, and increased risk of psychiatric comorbidity. Current treatment options for SAD are associated with low response rates, suboptimal efficacy, and possible risk of adverse effects. Investigation of new neurobiological mechanisms may aid in the identification of more specific therapeutic targets for the treatment of this disorder. Emerging evidence suggests that the endogenous cannabinoid system, also referred to as the endocannabinoid system (ECS), could play a potential role in the pathophysiology of SAD. This review discusses the known pathophysiological mechanisms of SAD, the potential role of the ECS in this disorder, current drugs targeting the ECS, and the potential of these novel compounds to enhance the therapeutic armamentarium for SAD. Further investigational efforts, specifically in human populations, are warranted to improve our knowledge of the ECS in SAD.

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“…1, Table 1), a receptor known to be involved in the neurobiology of anxiety (Petrie et al, 2021). In a broader sense, CB 1 R antagonism has been shown to reduce locomotor, exploratory, and rearing activity (Bogathy et al, 2019). Further studies using tests more sensitive to anxiety-related behaviors are needed.…”

Section: Behavior Effectsmentioning

confidence: 99%

GP120 and tenofovir alafenamide alter cannabinoid receptor 1 expression in hippocampus of mice

Kulbe

Mante

et al. 2023

Preprint

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Central nervous system (CNS) dysfunction remains prevalent in people with HIV (PWH) despite effective antiretroviral therapy (ART). There is evidence that low-level HIV infection and ART drugs may contribute to CNS damage in the brain of PWH with suppressed viral loads. As cannabis is used at a higher rate in PWH compared to the general population, there is interest in understanding how HIV proteins and ART drugs interact with the endocannabinoid system (ECS) and inflammation in the CNS. Therefore, we investigated the effects of the HIV envelope protein gp120 and tenofovir alafenamide (TAF) on cannabinoid receptor 1 (CB1R), glial fibrillary acidic protein (GFAP), and IBA1 in the brain and behavior in mice. The gp120 transgenic (tg) mouse model was administered TAF daily for 30 days and then analyzed using the open field test before being euthanized, and their brains were analyzed for CB1R, GFAP, and IBA1 expression using immunohistochemical approaches. CB1R, expression levels were significantly increased in CA1, CA2/3, and dentate gyrus of gp120tg mice compared to wt littermates; TAF reversed these effects. As expected, TAF showed a medium effect of enhancing GFAP in the frontal cortex of gp120tg mice in the frontal cortex. TAF had minimal effect on IBA1 signal. TAF showed medium to large effects on fine movements, rearing, total activity, total distance, and lateral activity in the open-field test. These findings suggest that TAF may reverse gp120-induced effects on CB1R expression and, unlike tenofovir disoproxil fumarate (TDF), may not affect gliosis in the brain.

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Blockade of Serotonin 2C Receptors with SB-242084 Moderates Reduced Locomotor Activity and Rearing by Cannabinoid 1 Receptor Antagonist AM-251

Cited by 7 publications

References 38 publications

Influence of the endocannabinoid system on the antidepressant activity of bupropion and moclobemide in the behavioural tests in mice

Influence of the endocannabinoid system on the antidepressant activity of bupropion and moclobemide in the behavioural tests in mice

The endocannabinoid system in social anxiety disorder: from pathophysiology to novel therapeutics

GP120 and tenofovir alafenamide alter cannabinoid receptor 1 expression in hippocampus of mice

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