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- | Preclinical, Journal: In Vivo and In Vitro Crosstalk Among CBD, A?, and Endocannabinoid System Enzymes and Receptors. (Pubmed Central) - Jun 5, 2025
elegans) strains. These insights advance our understanding of CBD's therapeutic potential in addressing neurodegenerative pathologies.
- | Journal: Coffee peel polyphenols ameliorate nonalcoholic fatty liver disease by modulating cannabinoid receptor type-1-ceramide axis. (Pubmed Central) - May 19, 2025
The reductions in hepatic ceramide concentrations contributed to down-regulating sterol regulatory element-binding protein-1c and up-regulating proliferator activated receptor alpha, leading to decrease de novo lipogenesis and increase fatty acid ?-oxidation in the liver, respectively. This study demonstrated a novel mechanism that CPPs could ameliorate NAFLD through modulating CB1-ceramide axis.
- | Journal: Profiling Allosteric Modulators of CB1R with an Allosteric Fluoroprobe. (Pubmed Central) - May 13, 2025
The utility of this work is highlighted by addressing ambiguities surrounding the binding of cannabidiol (CBD). CBD was found to interact with both allosteric and orthosteric sites of CB1R with comparable affinity (pKi = 5.34 and 5.67, respectively).
- | galantamine hydrobromide / Generic mfg., dantrolene / Generic mfg.
Journal: Computational approach for the evaluation of sesquiterpene lactone as a modulator of cannabinoid receptor type 2 for neurodegenerative disease prophylactics. (Pubmed Central) - Apr 28, 2025
CBD was found to interact with both allosteric and orthosteric sites of CB1R with comparable affinity (pKi = 5.34 and 5.67, respectively). Out of 85 sesquiterpene lactones evaluated, podachaenin (PubChem CID: 15,828,229) exhibited the highest binding affinity to CB2 (-?12.242
- | Journal: The synthetic cannabinoid agonist WIN 55,212-2 reduces experimental pruritus via CB2 receptor activation. (Pubmed Central) - Dec 10, 2024
In contrast, the sesquiterpene cannabis constituent ?-caryophyllene induced scratching, acting as a pruritogen. These preclinical data support the continuing investigation of cannabinoid receptor modulation as a potential therapeutic strategy for pruritus.
- | Journal: Extracellular glutamate is not modulated by cannabinoid receptor activity. (Pubmed Central) - Nov 11, 2024
Here, we measure the basal concentration of extracellular glutamate in layer 2/3 of mouse somatosensory cortex and find it to be 20-30 nM. We further examine the effect of cannabinoid receptor signaling on extracellular glutamate, and find no evidence for increased extracellular glutamate upon cannabinoid receptor agonist application.
- | Journal: The Endocannabinoid Peptide RVD-Hemopressin Is a TRPV1 Channel Blocker. (Pubmed Central) - Sep 29, 2024
Molecular docking and dynamics simulations indicated that RVD-Hp interacts with TRPV1's selectivity filter, forming stable hydrogen bonds and van der Waals contacts, thus preventing ion permeation. These findings highlight RVD-Hp's potential as a therapeutic agent for conditions involving TRPV1 activation, such as pain and anxiety.
- | Acomplia (rimonabant) / Sanofi
Journal: Modulation of CB1 cannabinoid receptor alters the electrophysiological properties of cerebellar Purkinje cells in harmaline-induced essential tremor. (Pubmed Central) - Sep 12, 2024
Male Wistar rats were assigned to control, harmaline (30?mg/kg), CBR agonist WIN 55,212-2 (WIN; 1?mg/kg), CB1R antagonists AM251 (1?mg/kg) and rimonabant (10?mg/kg)...However, CB1R antagonists provided protective effects against harmaline-induced electrophysiological changes in the spontaneous activity of PCs. Our findings reinforce the pivotal role of the endocannabinoid system in the underlying electrophysiological mechanisms of cerebellar disorders and suggest that antagonism of CB1R might provide therapeutic utility.
- ||| PepCan / University of Arkansas for Medical Sciences
Journal, Adverse events: MP-13, a novel chimeric peptide of morphiceptin and pepcan-9, produces potent antinociception with limited side effects. (Pubmed Central) - Sep 11, 2024
PERSPECTIVE: This article offers insights into the combination treatment of pepcans with morphiceptin. Among the chimeric peptides, MP-13 exhibited potent analgesic effects in a series of preclinical pain models with a favorable side-effect profile.
- | Journal: Structure-based identification of a G protein-biased allosteric modulator of cannabinoid receptor CB1. (Pubmed Central) - Jun 3, 2024
Notably, ago-BAM CB-05 demonstrated analgesic efficacy with fewer side effects, minimal drug toxicity and no cannabis addiction in mouse pain models. In summary, our finding not only suggests that ago-BAMs of CB1 provide a potential nonopioid strategy for pain management but also sheds light on BAM identification for GPCRs.
- | Journal: Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRABeCB2.0 Sensor. (Pubmed Central) - May 11, 2024
This current study expands upon the pharmacological characteristics of GRABeCB2.0 to enhance the understanding of fluorescent signal alterations in response to various functionally indiscriminate cannabinoid ligands. The results from this study could enhance the utility of the GRABeCB2.0 sensor for in vitro as well as in vivo studies of cannabinoid action and may aid in the development of novel ligands.
- | Journal: A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery. (Pubmed Central) - Dec 27, 2023
Representative ligands for CBRs, exhibiting diverse affinity and functional profiles, were utilized as reference compounds to validate the robustness and efficiency of the newly developed Tag-lite binding assay protocol. The homogeneous format, coupled with the sensitivity and optimal performance of the fluorescent ligand CELT-335, establishes this assay as a viable and reliable method for screening in hit and lead identification campaigns.
- | Journal: Beta-Caryophyllene, a Plant-Derived CB2 Receptor Agonist, Protects SH-SY5Y Cells from Cadmium-Induced Toxicity. (Pubmed Central) - Oct 28, 2023
Moreover, BCP treatment preserved cells from death, regulated the apoptosis pathway, and showed a significant anti-inflammatory effect, thus reducing the pro-inflammatory cytokines increased by the CdCl challenge. The results indicated that BCP preserved neuronal damage induced by Cd and might represent a future candidate for protection in neurotoxic conditions.
- Modulation of cannabinoid receptor-2 alters brain clearance of human tau (In-Person) - Jul 6, 2023 - Abstract #AAIC2023AAIC_4024;
The results indicated that BCP preserved neuronal damage induced by Cd and might represent a future candidate for protection in neurotoxic conditions. These studies will advance our understanding of the role of brain CB2 in pathologic tau removal and potentially highlight CB2 as a therapeutic target against tauopathies such as AD.
- | Journal: Platform Reagents Enable Synthesis of Ligand-Directed Covalent Probes: Study of Cannabinoid Receptor 2 in Live Cells. (Pubmed Central) - Jul 4, 2023
The LDC probes were characterized by a radioligand binding assay and TR-FRET experiments. Additionally, the probes were applied to specifically visualize CBR in conventional and imaging flow cytometry as well as in confocal fluorescence microscopy using overexpressing and endogenously expressing microglial live cells.
- || Review, Journal: Targeting the endocannabinoid system: structural determinants and molecular mechanism of allosteric modulation. (Pubmed Central) - May 13, 2023
We summarize newly synthesized AMs and the reported/predicted allosteric binding sites. We also discuss the structural determinants of the AMs binding as well as the molecular mechanism of CBR allostery.
- morphine sulphate / Generic mfg.
Investigating the effects of morphine and cannabidiol on pain sensitivity (Hall F-H (Indiana Convention Center)) - Feb 14, 2023 - Abstract #ACSSp2023ACS_SP_5237;
We also discuss the structural determinants of the AMs binding as well as the molecular mechanism of CBR allostery. Participant
- | Journal: Plasma-Derived Exosomes from NAFLD Patients Modulate the Cannabinoid Receptors' Expression in Cultured HepaRG Cells. (Pubmed Central) - Jan 22, 2023
Moreover, CB1R upregulation was associated with increased expression levels of PPAR-γ, a well-known mediator of liver tissue injury. In conclusion, this study provides evidence for CB1R transport by exosomes and suggests that the in vitro effects of circulating exosomes from NAFLD patients are mediated by the expression of cannabinoid receptors.
- | Journal: Low-Dose Administration of Cannabigerol Attenuates Inflammation and Fibrosis Associated with Methionine/Choline Deficient Diet-Induced NASH Model via Modulation of Cannabinoid Receptor. (Pubmed Central) - Jan 9, 2023
Collectively, the low dose of CBG alleviated hepatic fibrosis and inflammation in MCD-induced NASH, however, the high dose of CBG treatment showed enhanced liver damage when compared to MCD only group. These results will provide pre-clinical data to guide future intervention studies in humans addressing the potential uses of CBG for inflammatory liver pathologies, as well as open the door for further investigation into systemic inflammatory pathologies.
- | metamizole / Generic mfg., flurbiprofen / Generic mfg., ibuprofen / Generic mfg.
Journal: 2-Arylpropionic Acid Pyrazolamides as Cannabinoid CB2 Receptor Inverse Agonists Endowed with Anti-Inflammatory Properties. (Pubmed Central) - Dec 24, 2022
When subjected to functional testing on CB- or CB-transfected cells, compounds demonstrated an inverse agonist profile on CB receptors and the further characterization of compound LASSBio-2265 (11) revealed moderate binding affinity to CB receptor (K = 16 µM) with an EC = 0.36 µM (E = 63%). LASSBio-2265 (11) (at 1, 3, and 10 mg/kg p.o.) was investigated in the formalin test in mice and a remarkable analgesic activity in the late inflammatory phase was observed, suggesting it could be promising for the treatment of pain syndromes associated with chronic inflammatory diseases.
- || Review, Journal: Molecular Insights into Epigenetics and Cannabinoid Receptors. (Pubmed Central) - Nov 16, 2022
In this review, we discuss the significant research advances in different epigenetic factors contributing to the regulation of cannabinoid receptors and their functions under both physiological and pathological conditions. Increasing our understanding of the epigenetics of cannabinoid receptors will significantly advance our knowledge and could lead to the identification of novel therapeutic targets and innovative treatment strategies for diseases associated with altered cannabinoid receptor functions.
- | Journal: Development of an Indole-Amide-Based Photoswitchable Cannabinoid Receptor Subtype 1 (CBR) "Cis-On" Agonist. (Pubmed Central) - Aug 22, 2022
The novel compounds were evaluated by radioligand binding studies, receptor internalization, sensor receptor activation (GRABeCB2.0), Western blots for analysis of ERK1/2 activation, NanoBiT βarr2 recruitment, and calcium mobilization assays, respectively. The data show that the novel agonist 27a is a candidate for studying the optical modulation of cannabinoid receptors (CBRs), serving as a new molecular tool for investigating the involvement of hCBR in disorders associated with the endocannabinoid system.
- | Preclinical, Journal: Cannabidiol improves thyroid function via modulating vitamin D receptor in vitamin D deficiency diet-induced rat model. (Pubmed Central) - Jul 27, 2022
This is the first report with an improved CB2 and VDR expression after CBD treatment in VDD induced animals. Thus, CBD can be considered to use in hypothyroidism conditions and to maintain bone health.
- | Journal: Negative allosteric modulators of cannabinoid receptor 1: Ternary complexes including CB1, orthosteric CP55940 and allosteric ORG27569. (Pubmed Central) - Jul 23, 2022
These results suggest that the intracellular site might serve as an alternative binding site in CB1. Our studies show that the computational techniques we used are valuable in identifying ligand-binding pockets in proteins, and could be useful for the study of the interaction mode of other allosteric modulators.
- | Preclinical, Journal: Curcumin Protects Diabetic Mice against Isoproterenol-Induced Myocardial Infarction by Modulating CB2 Cannabinoid Receptors. (Pubmed Central) - May 30, 2022
However, the AM630 pre-treatment attenuated the effects of curcumin. The data suggest the involvement of CB2R in the actions of curcumin such as in the prevention of myocardial stress and in the improvement of the normal status of the myocardial membrane associated with diabetes.
- | Journal: Topical application of cannabinoid-ligands ameliorates experimental dry-eye disease. (Pubmed Central) - Apr 29, 2022
The data suggest the involvement of CB2R in the actions of curcumin such as in the prevention of myocardial stress and in the improvement of the normal status of the myocardial membrane associated with diabetes. Endocannabinoid receptor modulation presents a potential multi-functional therapeutic approach for DED.
- || Preclinical, Review, Journal: On the Biomedical Properties of Endocannabinoid Degradation and Reuptake Inhibitors: Pre-clinical and Clinical Evidence. (Pubmed Central) - Mar 31, 2022
For this purpose, we revisited the available literature and reported the latest advances regarding the biomedical properties of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors in pre-clinical and clinical studies. We also highlighted anandamide and 2-arachidonoylglycerol reuptake inhibitors with promising results in pre-clinical studies using in vitro and animal models as an outlook for future research in clinical trials.
- || Preclinical, Retrospective data, Review, Journal: Association of cannabinoid receptor modulation with normal and abnormal skeletal remodelling: A systematic review and meta-analysis of in vitro, in vivo and human studies. (Pubmed Central) - Mar 19, 2022
Thus, CB1/2 modulation is associated with altered bone metabolism, however findings are confounded by low study number and heterogenicity of models. DATA AVAILABILITY: The datasets used and analysed in the present study are available from the public sources described.
- | Journal: Distinct Binding Mechanisms for Allosteric Sodium Ion in Cannabinoid Receptors. (Pubmed Central) - Mar 5, 2022
Furthermore, simulations also show that intracellular Na could bind to the Na binding site in CB. Constructed Markov state models show that the standard free energy of Na binding is similar to the previously calculated free energy for other class A GPCRs.
- || Review, Journal: Cannabinoid-induced changes in the immune system: The role of microRNAs. (Pubmed Central) - Feb 2, 2022
Such studies have highlighted the key role played by various miRNAs in driving the observed immunomodulatory effects of cannabinoids. The aim of this review article, therefore, is to summarize the role of miRNAs behind the observed effects of cannabinoids on the overall immune system, rather than focusing on a single disease state.
- Fluorescent and photoswitchable probes for targeted study of cannabinoid receptors (Sapphire E/F (Hilton San Diego Bayfront)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_11707;
Stereodivergent synthesis of azobenzene-substituted THC derivatives enabled the first example of reversible optical control over CB1 signaling, as demonstrated by whole-cell electrophysiology. A related approach accessed photoswitchable derivatives of CB2 agonist HU-308, allowing for the optical control over CB2-mediated Ca2+ transients in AtT-20(CB2) cells.
- | Journal: CB1 receptor binding sites for NAM and PAM: a first approach for studying, new n-butyl-diphenylcarboxamides as allosteric modulators. (Pubmed Central) - Jan 27, 2022
Computational studies were performed to investigate the role of these compounds in CB1R modulation. The analysis of their binding poses in two different binding cavities of the CB1R surface, revealed a preferred interaction with the experimental binding site for negative allosteric modulators.
- || Sativex (nabiximols) / Jazz, Epidiolex (cannabidiol) / Jazz
Clinical, Review, Journal: Food Effects on the Formulation, Dosing, and Administration of Cannabidiol (CBD) in Humans: A Systematic Review of Clinical Studies. (Pubmed Central) - Jan 7, 2022
Clinical trials focusing on the performance of Epidiolex, the FDA-approved CBD formulation, were found in several databases and systematically analyzed in terms of administration method, dosing schedules, and patient characteristics...Considering all the different oral formulations of CBD, further analysis points to the main excipient of oral CBD formulations (refined sesame seed oil) as a major contributor to the dose-dependent variations in CBD pharmacokinetics, especially affecting the fasted state. We discuss the implications of these results on the downstream pharmacodynamics of endocannabinoid receptor modulation and its broad physiological implications.
- | PepCan / University of Arkansas for Medical Sciences
Preclinical, Journal: Characterization of pepcan-23 as pro-peptide of RVD-hemopressin (pepcan-12) and stability of hemopressins in mice. (Pubmed Central) - Jan 1, 2022
Overall, we show that pepcan-23 is a biological pro-peptide of RVD-hemopressin and divalent metal ions may regulate this process. Given the lack of metabolic stability of hemopressins, administration of pepcan-23 as pro-peptide may be suitable in pharmacological experiments as it is converted to RVD-hemopressin in vivo.
- Cannabinoid receptor modulation of Cav3.2 voltage-gated calcium channels (Virtual Only) - Dec 20, 2021 - Abstract #Neuroscience2021Neuroscience_4798;
These results are the first indication that cannabinoid receptors can alter Cav3.2 channel gating to decrease the size of the window current. Future experiments will determine whether this is a result of constitutive activity of CB1R on Cav3.2, or a potential physical interaction between these two channels.; Grant Support: Eyes High Postdoctoral Fellowship; Alberta Innovates mCannabis Program
- | Journal: Dopaminergic denervation impairs cortical motor and associative/limbic information processing through the basal ganglia and its modulation by the CB1 receptor. (Pubmed Central) - Dec 16, 2021
Moreover, although DA denervation does not change CB1 receptor density, it impairs its functionality, leading to a lack of modulation. These data highlight an abnormal transfer of information through the associative/limbic domains after DA denervation that may be related to the non-motor symptoms manifested by Parkinson's disease patients.
- | Journal: Cholesterol as a modulator of cannabinoid receptor CB signaling. (Pubmed Central) - Dec 16, 2021
The differential effects of a specific ligand on activation of CB in different types of membranes may have implications for screening of drug candidates in a search of modulators of GPCR activity. MD simulation suggests that cholesterol exerts an allosteric effect on the intracellular regions of the receptor that interact with the G-protein complex thereby altering the recruitment of G protein.
- | Journal: Cannabinoid receptor interacting protein 1a (CRIP1a) interacts with myristoylated Gα-N-terminus via a unique gapped β-barrel structure. (Pubmed Central) - Nov 21, 2021
However, CRIP1a could not bind the non-myristolyated Gα peptide or cargo of homologs. Thus, binding of CRIP1a to Gαi proteins represents a novel mechanism to regulate cell signaling initiated by the CB receptor.
- || Review, Journal: Antipsychotics cardiotoxicity: What's known and what's next. (Pubmed Central) - Nov 6, 2021
We also provide an up-to-date perspective on future clinical monitoring and therapeutic strategies for antipsychotic cardiotoxicity. We propose that third-generation antipsychotics or drug adjuvant therapy, such as cannabinoid receptor modulators that confer dual benefits - i.e., alleviating cardiotoxicity and improving metabolic disorders - deserve further clinical evaluation and marketing.
- | morphine sulphate / Generic mfg.
Journal: Cannabinoid receptor modulation changes the accumbal neuronal responses to morphine in the reinstatement of morphine-induced conditioned place preference. (Pubmed Central) - Sep 30, 2021
The inhibitory effect of cannabinoid on the NAc neuronal activity in the reinstatement has indicated the possible potency of cannabinoid to induce reinstatement of morphine-induced CPP alone and in the absence of a priming dose of morphine. Also, the different effects of the CB1 agonist during the extinction period in the reinstatement phase suggest different mechanisms underlying these two parts.
- || Review, Journal: Modern Approaches to the Development of Synthetic Cannabinoid Receptor Probes. (Pubmed Central) - Sep 16, 2021
We also describe structural classes of positive- and negative allosteric modulators (PAMs and NAMs) of CB1R and CB2R. Finally, we introduce new opportunities for cannabinoid receptor probe development that have emerged in recent years, including biased agonists that may lead to medications lacking adverse effects.
- | Journal: Novel Machaeriol Analogues as Modulators of Cannabinoid Receptors: Structure-Activity Relationships of (+)-Hexahydrocannabinoids and Their Isoform Selectivities. (Pubmed Central) - Aug 17, 2021
For the first time, with the aid of structure-activity relationships of (+)-hexahydrocannabinoids, CB selective agonists were identified with late-stage diversification using palladium-mediated C-C bond formation. By simply switching to (R)-citronellal as a chiral precursor, enantiomerically pure (-)-hexahydrocannabinoids with better CB/CB receptor isoform selectivity can be obtained using the current synthetic approach.
- | Preclinical, Journal: Cannabinoid Receptor Modulation of Neurogenesis: ST14A Striatal Neural Progenitor Cells as a Simplified In Vitro Model. (Pubmed Central) - Jun 22, 2021
Phospholipase C (PLC), but not PI3K pharmacological blockade negatively modulated CB2-induced ST14A cell proliferation, suggesting that a PLC pathway is involved in the steps downstream to CB2 activation. On the basis of our results, we propose ST14A neural progenitor cells as a useful in vitro model for studying ECS modulation of neurogenesis, also in prospective in vivo pharmacological studies.
- | Journal: Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. (Pubmed Central) - Jun 2, 2021
Interestingly, compound 24 proved to be able to activate both cannabinoid and TRPV1 receptors. Even if cannabinoid receptor subtype selectivity remained a goal only partially achieved, results confirm the validity of the alkylresorcinol nucleus as skeleton for the identification of potent cannabinoid receptor modulators.
- | Journal: Allosteric Modulation of the CB1 Cannabinoid Receptor by Cannabidiol-A Molecular Modeling Study of the N-Terminal Domain and the Allosteric-Orthosteric Coupling. (Pubmed Central) - May 25, 2021
In addition, we identified the changes in the orthosteric binding mode of Δ-THC, as well as the changes in its binding energy, caused by the CBD allosteric binding. We have also found that the presence of a complete N-terminal domain is essential for a stable binding of CBD in the allosteric site of CBR as well as for the allosteric-orthosteric coupling mechanism.
- | Acomplia (rimonabant) / Sanofi
Journal: WIN55,212-2, a Dual Modulator of Cannabinoid Receptors and G Protein-Coupled Inward Rectifier Potassium Channels. (Pubmed Central) - May 1, 2021
Interestingly, the inward rectifier potassium channel, IRK1, a non-G protein-coupled potassium channel important for setting the resting membrane voltage and highly similar to GIRK1 and GIRK2, is not sensitive to WIN55,212-2, Δ9-THC, CBD, CP55,940, or rimonabant. From this, it is concluded that WIN55,212-2 selectively blocks GIRK1/2.
- | Journal: LPS-mediated neutrophil VEGF-A release is modulated by cannabinoid receptor activation. (Pubmed Central) - Mar 25, 2021
We demonstrated that low concentrations of CB agonists inhibit VEGF-A release from LPS-activated PMNs. These results suggest that CB agonists might represent a novel therapeutic strategy in patients with sepsis.
- | Journal: Negative Allosteric Modulators of Cannabinoid Receptor 2: Protein Modeling, Binding Site Identification and Molecular Dynamics Simulations in the Presence of an Orthosteric Agonist. (Pubmed Central) - Dec 30, 2020
Binding of either TBC or DHGA to a putative allosteric pocket directly adjacent to the orthosteric ligand reduced the binding free energy of CP55,940, which is consistent with the expected effect of a negative AM. The identified allosteric sites present immense scope for the discovery of novel classes of CB2 allosteric modulators.
- || Review, Journal: New Insights Into Peptide Cannabinoids: Structure, Biosynthesis and Signaling. (Pubmed Central) - Dec 29, 2020
The novel peptide compounds derived from hemoglobin chains and their non-classical activation of cannabinoid receptors are only starting to be uncovered. It will be exciting to follow the ensuing discoveries, not only in reference to what is already known of the classical lipid endocannabinoids revealing more complex aspects of endocannabinoid system, but also as to its possibilities as a future therapeutic tool.
- | Journal: Early-life stress exacerbates the effects of WIN55,212-2 and modulates the cannabinoid receptor type 1 expression. (Pubmed Central) - Dec 5, 2020
Moreover, CB-positive fibres were reduced in limbic areas in MSEW mice after cannabinoid withdrawal precipitated with the CB antagonist SR141617A. These findings support that early-life stress promotes behavioural and molecular changes in the sensitivity to cannabinoids, which are mediated by alterations in CB signalling in limbic areas and it induces an increased Iba1-microglial marker which could interfere in emotional memories formation.