Negative allosteric modulators of cannabinoid receptor 1: Ternary complexes including CB1, orthosteric CP55940 and allosteric ORG27569

Aderibigbe, AyoOluwa O.; Pandey, Pankaj; Doerksen, Robert J.

doi:10.1080/07391102.2021.1873187

Cited by 5 publications

(3 citation statements)

References 85 publications

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“…-Reduces cocaine and methamphetamine seeking behaviour in rat model -Hypophagic, and thus may have use in the treatment of obesity [339][340][341][342][343][344] Peripheral CB 1 R agonists do not cross the blood-brain barrier (BBB), and are suggested to circumvent the psychotropic effects and other adverse side-effects such as cardiovascular and immune perturbations produced by CB 1 R activation. Examples of peripheral CB 1 R agonists (aka peripherally restricted cannabinoid 1 receptor (PRCB)) are listed in Table 7.…”

Section: Gat228 (R-enantiomer)mentioning

confidence: 99%

The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases

Lowe

Toyang²,

Steele

et al. 2021

IJMS

160

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The Endocannabinoid System (ECS) is primarily responsible for maintaining homeostasis, a balance in internal environment (temperature, mood, and immune system) and energy input and output in living, biological systems. In addition to regulating physiological processes, the ECS directly influences anxiety, feeding behaviour/appetite, emotional behaviour, depression, nervous functions, neurogenesis, neuroprotection, reward, cognition, learning, memory, pain sensation, fertility, pregnancy, and pre-and post-natal development. The ECS is also involved in several pathophysiological diseases such as cancer, cardiovascular diseases, and neurodegenerative diseases. In recent years, genetic and pharmacological manipulation of the ECS has gained significant interest in medicine, research, and drug discovery and development. The distribution of the components of the ECS system throughout the body, and the physiological/pathophysiological role of the ECS-signalling pathways in many diseases, all offer promising opportunities for the development of novel cannabinergic, cannabimimetic, and cannabinoid-based therapeutic drugs that genetically or pharmacologically modulate the ECS via inhibition of metabolic pathways and/or agonism or antagonism of the receptors of the ECS. This modulation results in the differential expression/activity of the components of the ECS that may be beneficial in the treatment of a number of diseases. This manuscript in-depth review will investigate the potential of the ECS in the treatment of various diseases, and to put forth the suggestion that many of these secondary metabolites of Cannabis sativa L. (hereafter referred to as “C. sativa L.” or “medical cannabis”), may also have potential as lead compounds in the development of cannabinoid-based pharmaceuticals for a variety of diseases.

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Section: Gat228 (R-enantiomer)mentioning

confidence: 99%

The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases

Lowe

Toyang²,

Steele

et al. 2021

IJMS

160

View full text Add to dashboard Cite

show abstract

“…This site had been determined by prior computational studies—using computational docking, Glide docking scores, binding free energy calculations, and extensive molecular dynamics (MD) simulations—to be the second most likely binding site for Org27569. These findings highlight the dynamic nature of receptor–ligand interactions and the crucial role of structural studies in verifying theoretical models [ 65 ].…”

Section: Research Main Overview: the Endocannabinoid System With Cann...mentioning

confidence: 99%

Cannabinoids: Potential for Modulation and Enhancement When Combined with Vitamin B12 in Case of Neurodegenerative Disorders

Kaszyńska

2024

Pharmaceuticals

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The enduring relationship between humanity and the cannabis plant has witnessed significant transformations, particularly with the widespread legalization of medical cannabis. This has led to the recognition of diverse pharmacological formulations of medical cannabis, containing 545 identified natural compounds, including 144 phytocannabinoids like Δ9-THC and CBD. Cannabinoids exert distinct regulatory effects on physiological processes, prompting their investigation in neurodegenerative diseases. Recent research highlights their potential in modulating protein aggregation and mitochondrial dysfunction, crucial factors in conditions such as Alzheimer’s Disease, multiple sclerosis, or Parkinson’s disease. The discussion emphasizes the importance of maintaining homeodynamics in neurodegenerative disorders and explores innovative therapeutic approaches such as nanoparticles and RNA aptamers. Moreover, cannabinoids, particularly CBD, demonstrate anti-inflammatory effects through the modulation of microglial activity, offering multifaceted neuroprotection including mitigating aggregation. Additionally, the potential integration of cannabinoids with vitamin B12 presents a holistic framework for addressing neurodegeneration, considering their roles in homeodynamics and nervous system functioning including the hippocampal neurogenesis. The potential synergistic therapeutic benefits of combining CBD with vitamin B12 underscore a promising avenue for advancing treatment strategies in neurodegenerative diseases. However, further research is imperative to fully elucidate their effects and potential applications, emphasizing the dynamic nature of this field and its potential to reshape neurodegenerative disease treatment paradigms.

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“…3CLpro cuts multiple proteins at 11 different sites to generate various non-structural proteins that are important for virus replication. This major protease binds viral particles to the capsid protein shell and prevents the increase of viral load in the host cell, which is critical for the viral life cycle, making it an attractive target for anti-SARS-CoV-2 inhibitors [6] . Therefore, 3CLPro is considered a prime target for the treatment of SARS-CoV-2 infection.…”

Section: Introductionmentioning

confidence: 99%

Molecular design, molecular docking and ADMET study of cyclic sulfonamide derivatives as SARS-CoV-2 inhibitors

Tong

Zhang

Luo

et al. 2021

Chinese Journal of Analytical Chemistry

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Negative allosteric modulators of cannabinoid receptor 1: Ternary complexes including CB1, orthosteric CP55940 and allosteric ORG27569

Cited by 5 publications

References 85 publications

The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases

The Endocannabinoid System: A Potential Target for the Treatment of Various Diseases

Cannabinoids: Potential for Modulation and Enhancement When Combined with Vitamin B12 in Case of Neurodegenerative Disorders

Molecular design, molecular docking and ADMET study of cyclic sulfonamide derivatives as SARS-CoV-2 inhibitors

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