Differences in receptor binding affinity of several phytocannabinoids do not explain their effects on neural cell cultures

Rosenthaler, Sarah; Pöhn, Birgit; Kolmanz, Caroline; Nguyen, Chi Huu; Krewenka, Christopher; Huber, Alexandra; Kranner, Barbara; Rausch, Wolf‐Dieter; Moldzio, Rudolf

doi:10.1016/j.ntt.2014.09.003

Cited by 116 publications

(114 citation statements)

References 31 publications

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“…CBG has low affinity for the cannabinoid CB 1 and CB 2 receptors [58–60], but it affects the endocannabinoid system because of its ability to inhibit anandamide (AEA) uptake [29]. CBG has also been shown to weakly inhibit the LPI response in GPR55 assays [18].…”

Section: Pharmacology Of Selected Phytocannabinoidsmentioning

confidence: 99%

“…This phytocannabinoid does not display significant affinity for the cannabinoid CB 1 and CB 2 receptors [58]. Nonetheless, it directly influences the endocannabinoid system by inhibiting anandamide (AEA) uptake [29].…”

Section: Pharmacology Of Selected Phytocannabinoidsmentioning

confidence: 99%

“…This compound displays very weak affinity for CB 1 and CB 2 receptors [58, 71]. Its ability to inhibit the activity of the putative endogenous ligand LPI has been reported in h GPR55-HEK293 cells [18].…”

Section: Pharmacology Of Selected Phytocannabinoidsmentioning

confidence: 99%

See 2 more Smart Citations

Molecular Targets of the Phytocannabinoids: A Complex Picture

Morales

Hurst

Reggio

2017

Progress in the Chemistry of Organic Natural Products

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353

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Section: Pharmacology Of Selected Phytocannabinoidsmentioning

confidence: 99%

Section: Pharmacology Of Selected Phytocannabinoidsmentioning

confidence: 99%

See 1 more Smart Citation

Molecular Targets of the Phytocannabinoids: A Complex Picture

Morales

Hurst

Reggio

2017

Progress in the Chemistry of Organic Natural Products

331

353

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“…-Tetrahydrocannabinolic acid (⌬ 9 -THCA) was recently reported to have moderate affinity for human CB1 (K i 23 nM) and CB2 (K i 56 nM) receptors (742), although previous data (6, 879) strongly contradict this finding. ⌬ 9 -THCA is a weak TRPA1 agonist (EC 50 2.7 M) and a good TRPM8 antagonist (IC 50 0.15 M) (193), and is antiproliferative against cancer cells (478) and antispasmodic (860).…”

mentioning

confidence: 95%

From Phytocannabinoids to Cannabinoid Receptors and Endocannabinoids: Pleiotropic Physiological and Pathological Roles Through Complex Pharmacology

Ligresti¹,

Petrocellis²,

Marzo³

2016

Physiological Reviews

378

337

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Apart from having been used and misused for at least four millennia for, among others, recreational and medicinal purposes, the cannabis plant and its most peculiar chemical components, the plant cannabinoids (phytocannabinoids), have the merit to have led humanity to discover one of the most intriguing and pleiotropic endogenous signaling systems, the endocannabinoid system (ECS). This review article aims to describe and critically discuss, in the most comprehensive possible manner, the multifaceted aspects of 1) the pharmacology and potential impact on mammalian physiology of all major phytocannabinoids, and not only of the most famous one ⌬ 9 -tetrahydrocannabinol, and 2) the adaptive prohomeostatic physiological, or maladaptive pathological, roles of the ECS in mammalian cells, tissues, and organs. In doing so, we have respected the chronological order of the milestones of the millennial route from medicinal/recreational cannabis to the ECS and beyond, as it is now clear that some of the early steps in this long path, which were originally neglected, are becoming important again. The emerging picture is rather complex, but still supports the belief that more important discoveries on human physiology, and new therapies, might come in the future from new knowledge in this field.

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“…CBDA has been shown to be an inhibitor of cell migration in the highly aggressive human breast cancer MDA-MB-231 by alteration of Rho GTPase activity (Takeda et al, 2012). CBDV, the C4′-propyl analog of CBD, displays very weak affinity for CB 1 and CB 2 receptors (Hill et al, 2013; Rosenthaler et al, 2014), whereas it has been reported to inhibit the activity of the putative endogenous ligand LPI in h GPR55-HEK293 cells (Anavi-Goffer et al, 2012). CBDV also targets the human TRPA1 channel (De Petrocellis et al, 2011, 2012).…”

Section: Natural Cannabidiol Derivativesmentioning

confidence: 99%

An Overview on Medicinal Chemistry of Synthetic and Natural Derivatives of Cannabidiol

2017

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Cannabidiol (CBD) has been traditionally used in Cannabis-based preparation, however historically, it has received far less interest as a single drug than the other components of Cannabis. Currently, CBD generates considerable interest due to its beneficial neuroprotective, antiepileptic, anxiolytic, antipsychotic, and anti-inflammatory properties. Therefore, the CBD scaffold becomes of increasing interest for medicinal chemists. This review provides an overview of the chemical structure of natural and synthetic CBD derivatives including the molecular targets associated with these compounds. A clear identification of their biological targets has been shown to be still very challenging.

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Differences in receptor binding affinity of several phytocannabinoids do not explain their effects on neural cell cultures

Cited by 116 publications

References 31 publications

Molecular Targets of the Phytocannabinoids: A Complex Picture

Molecular Targets of the Phytocannabinoids: A Complex Picture

From Phytocannabinoids to Cannabinoid Receptors and Endocannabinoids: Pleiotropic Physiological and Pathological Roles Through Complex Pharmacology

An Overview on Medicinal Chemistry of Synthetic and Natural Derivatives of Cannabidiol

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