Behavioral assessment of rimonabant under acute and chronic conditions

Ettaro, Robert; Laudermilk, Lucas; Clark, Stewart D.; Maitra, Rangan

doi:10.1016/j.bbr.2020.112697

Cited by 21 publications

(18 citation statements)

References 37 publications

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“…Studies have shown that SR-1417116A (i.p.) does not affect the decreased locomotor activity induced by CB1receptor agonists, increases locomotor activity or inhibits it [14, 15,16]. Our results support the findings of a study where SR-141716 (i.p.)…”

Section: Discussionsupporting

confidence: 90%

Cb1-Receptor Antagonist Sr-141716a Modulates Locomotor Activity in Obx-Rats

Velikova¹,

Doncheva²,

Tashev³

2022

JofIMAB

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Dysfunction of the endocannabinoid system has been related to depressive-like behavior. In our study, bilateral olfactory bulbectomy (OBX) was used as an animal model of depression. We evaluated the effect of the selective CB1-antagonist SR-141716A (Rimonabant) on the exploratory and locomotor activity of OBX-rats. Rimonabant was administered intragastrically for 14 days to OBX-rats, divided into 3 experimental groups, where the drug was given before; immediately (1-14 days) after; or 14 days (14-28 day) after OBX. Exploratory and locomotor activity of OBX-rats was tested in an Opto-Varimex apparatus. SR-141716A, administered subchronically, intragastrically exerted locomotor stimulating effects in OBX- and sham-operated rats, while the exploratory activity was not affected. The time interval for the drug administration is of significance for the manifestation of the effects on locomotor activity in OBX-rats. SR-141716A applied 14 days before OBX or after the development of a depressive-like state (14-28 days after OBX), but not immediately after OBX (1-14 days) aggravated the OBX-induced hyperlocomotor state.

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Section: Discussionsupporting

confidence: 90%

Cb1-Receptor Antagonist Sr-141716a Modulates Locomotor Activity in Obx-Rats

Velikova¹,

Doncheva²,

Tashev³

2022

JofIMAB

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“…For instance, rimonabant, the first inverse agonist of CB 1 approved for obese patients, was withdrawn from the market due to adverse effects related to the central nervous system, including depression and suicidal ideation. However, it has recently been shown that the chronic administration of rimonabant in rats was not associated with development of adverse psychiatric phenotypes, suggesting that the analysis of a patient’s comorbidity, such as obesity, is fundamental to prevent this (and other possible) side effect [ 53 ]. Moreover, the efficacy and safety of lenabasum, a novel oral CB 2 agonist, is currently under investigation in multiple autoimmune and fibrotic diseases, including SLE and systemic sclerosis [ 54 ].…”

Section: Discussionmentioning

confidence: 99%

2-Arachidonoylglycerol Reduces the Production of Interferon-Gamma in T Lymphocytes from Patients with Systemic Lupus Erythematosus

et al. 2022

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Background: the endocannabinoid 2-arachidonoylglycerol (2-AG) plays a pivotal role in immune cells regulation. The plasma levels of 2-AG are increased in patients with systemic lupus erythematosus (SLE) and correlate with disease activity. Moreover, in plasmacytoid dendritic cells from SLE patients, 2-AG is able to control the production of type 1 interferon (IFN) through CB2 activation. The aim of this study was to evaluate the potential role of 2-AG on T lymphocytes from SLE patients. Methods: peripheral blood mononuclear cells (PBMCs) from SLE participants and age- and sex-matched healthy donors (HD) were isolated by Ficoll–Hypaque density-gradient centrifugation. The PBMCs were treated with increasing concentrations of 2-AG, and AM251 and AM630 were used to antagonize CB1 and CB2, respectively. Flow cytometry was used to assess the expression of CD3, CD4, CD8, CD25, IFN-ɣ, IL-4, and IL-17A. Results: 2-AG (1 μM) decreased IFN-ɣ expression (p = 0.0005) in the Th1 lymphocytes of SLE patients. 2-AG did not modulate the cytokine expression of any other T lymphocyte population from either SLE or HD. Treatment with both 2-AG and AM630 increased the IFN-ɣ expression in Th1 lymphocytes of SLE patients (p = 0.03). Discussion: 2-AG is able to modulate type 2 IFN production from CD4+ T lymphocytes from SLE patients through CB2 activation.

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“…Targeted activation of CB1 may bring some side effects to the CNS, such as depression, suicidal tendency, and other mental disorders (79). However, activation of CB2 receptor does not cause these central side effects.…”

Section: Endocannabinoid System and Microglial Functions In Autismmentioning

confidence: 99%

Endocannabinoid System Unlocks the Puzzle of Autism Treatment via Microglia

Yan

et al. 2021

Front. Psychiatry

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Autism spectrum disorder (ASD) is a serious neurodevelopmental disorder and characterized by early childhood-onset impairments in social interaction and communication, restricted and repetitive patterns of behavior or interests. So far there is no effective treatment for ASD, and the pathogenesis of ASD remains unclear. Genetic and epigenetic factors have been considered to be the main cause of ASD. It is known that endocannabinoid and its receptors are widely distributed in the central nervous system, and provide a positive and irreversible change toward a more physiological neurodevelopment. Recently, the endocannabinoid system (ECS) has been found to participate in the regulation of social reward behavior, which has attracted considerable attention from neuroscientists and neurologists. Both animal models and clinical studies have shown that the ECS is a potential target for the treatment of autism, but the mechanism is still unknown. In the brain, microglia express a complete ECS signaling system. Studies also have shown that modulating ECS signaling can regulate the functions of microglia. By comprehensively reviewing previous studies and combining with our recent work, this review addresses the effects of targeting ECS on microglia, and how this can contribute to maintain the positivity of the central nervous system, and thus improve the symptoms of autism. This will provide insights for revealing the mechanism and developing new treatment strategies for autism.

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Behavioral assessment of rimonabant under acute and chronic conditions

Cited by 21 publications

References 37 publications

Cb1-Receptor Antagonist Sr-141716a Modulates Locomotor Activity in Obx-Rats

Cb1-Receptor Antagonist Sr-141716a Modulates Locomotor Activity in Obx-Rats

2-Arachidonoylglycerol Reduces the Production of Interferon-Gamma in T Lymphocytes from Patients with Systemic Lupus Erythematosus

Endocannabinoid System Unlocks the Puzzle of Autism Treatment via Microglia

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