PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor

Meini, Serena; Gado, Francesca; Stevenson, Lesley; Digiacomo, Maria; Codini, Simone; Macchia, Marco; Pertwee, Roger Guy; Manera, Clementina

doi:10.1016/j.ejmech.2020.112606

Cited by 3 publications

(1 citation statement)

References 35 publications

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“…This modulation is particularly valuable in medical conditions associated with excessive CB 1 R activation, providing a targeted approach to mitigating adverse effects of cannabinoid overactivity. The unique properties of PSNCBAM-1 highlight its potential therapeutic applications in managing disorders linked to cannabinoid receptor dysregulation [ 68 , 69 ].…”

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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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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CB1 allosteric modulators and their therapeutic potential in CNS disorders

Mielnik

Lam

Ross

2021

Progress in Neuro-Psychopharmacology and Biological Psychiatry

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Maxdo and RDF55v are Crucial Molecular Descriptors Governing the Cannabinoid Receptor 1(CB1) Modulator Activity of N, N'-diphenyl Urea Analogs and 1H-Indole-2-carboxamides

Lone,

Begum,

Khanday

2024

Orient. J. Chem

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CB1 allosteric modulators such as synthetic cannabinoids are promising therapeutic agents. Among the various CB1 receptor modulators, indole-2-carboxamides, and N, N'-diphenyl urea derivatives are continuously explored for their potency and selectivity towards the receptor. In the present computational work, QSAR models were generated using Drug Theoretics and Chemoinformatics (DTC tools) tools to analyze the influence of molecular features of these modulators (one hundred and fourteen compounds) on the activity. A statistically significant three-parameter model (SPMin2_Bhm, maxdO, and minssN) was derived that displayed R2 and Q2 values of 0.66 and 0.62, respectively. SPMin2_Bhm and maxdO negatively correlated with the activity, whereas minssN has a positive connection. A seven-parameter model (maxdO, minsssN, RDF55v, VE3_D, minHBint10, SpMin5_Bhs, and CrippenLogP) was also obtained with R2 and Q2 values of 0.76 and 0.70, respectively. The findings might assist in the design and development of novel CB1 modulators based on the structures of indole-2-carboxamides and N, N'-diphenyl urea

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PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor

Cited by 3 publications

References 35 publications

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

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

CB1 allosteric modulators and their therapeutic potential in CNS disorders

Maxdo and RDF55v are Crucial Molecular Descriptors Governing the Cannabinoid Receptor 1(CB1) Modulator Activity of N, N'-diphenyl Urea Analogs and 1H-Indole-2-carboxamides

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