CB-2

BACKGROUND: The elevation of endocannabinoid levels through inhibiting their degradation afforded neuroprotection in CaMKIIα-TDP-43 mice, a conditional transgenic model of frontotemporal dementia. However, which cannabinoid receptors are mediating these benefits is still pending to be elucidated. METHODS: We have investigated the involvement of the CB1 and the CB2 receptor using chronic treatments with selective ligands in CaMKIIα-TDP-43 mice, analysis of their cognitive deterioration with the Novel Object Recognition test, and immunostaining for neuronal and glial markers in two areas of interest in frontotemporal dementia...

Cannabinoid CB 2 agonists show therapeutic efficacy without the unwanted side effects commonly associated with direct activation of CB 1 receptors. The G protein-biased CB 2 receptor agonist LY2828360 attenuates the maintenance of chemotherapy-induced neuropathic nociception in male mice and blocks the development of morphine tolerance in this model. However, the specific cell types involved in this phenomenon have never been investigated and whether this therapeutic profile is observed in female mice remains poorly understood...

UNLABELLED: Sensometrics assesses sensory perspectives in consumer research using statistics and various methodologies. This study evaluated consumer responses to hot and cold germinated-wheat beverages in check-all-that-apply (CATA) and rate-all-that-apply (RATA) assessments using sensometric statistical approaches, including Cochran's Q test, penalty-lift analysis, and multiple factor analysis. Hot beverages (HB) were prepared by infusion using different amounts of germinated wheat (HB_1: 0...

A comprehensive study on the synthesis and characterization of NHC-ligated nickel(II) cyanoborates (CBs) is presented (NHC = N-heterocyclic carbene). Nickel(II) cyanoborates Ni[BH2 (CN)2 ]2 ·H2 O (Ib·H2 O), Ni[BH(CN)3 ]2 ·0.5H2 O (Ic·0.5H2 O), Ni[B(CN)4 ]2 ·H2 O (Id·H2 O) were reacted with selected NHCs of different steric size. The reaction of the nickel cyanoborates with small to medium-sized NHCs Me2 ImMe and iPr2 Im (R2 Im = 1,3-di-organyl-imidazolin-2-ylidene; R2 ImMe = 1,3-di-organyl-4,5-dimethyl-imidazolin-2-ylidene) afforded cyanoborate salts containing the rare homoleptic fourfold NHC-ligated nickel(II) cations [Ni(NHC)4 ]2+ (NHC = Me2 ImMe (1c-d), iPr2 Im (2c-d)) and cyanoborate counter-anions...

(1) Background: Structural remodeling plays an important role in the pathophysiology of atrial fibrillation (AF). It is likely that structural remodeling occurs transmurally, giving rise to electrical endo-epicardial asynchrony (EEA). Recent studies have suggested that areas of EEA may be suitable targets for ablation therapy of AF. We hypothesized that the degree of EEA is more pronounced in areas of transmural conduction block (T-CB) than single-sided CB (SS-CB). This study examined the degree to which SS-CB and T-CB enhance EEA and which specific unipolar potential morphology parameters are predictive for SS-CB or T-CB...

Application of biosolids to agricultural land has gained increasing attention due to their rich nutrient content. There are a variety of treatment processes for converting sewage sludge to biosolids. Different treatment processes can change the physicochemical properties of the raw sewage sludge and affect the dynamics of nutrient release in biosolids-amended soils. This paper reviews heat drying, alkaline treatment, and composting as biosolids treatment processes and discusses the effects of these treatments on biosolid nitrogen (N) content and availability...

(1) Background: Considering that the specialty literature supplies only general data about the variability of the cervical branch of the facial nerve, this study aimed to determine this branch's variation and individual peculiarities depending on the nerve branching pattern and anthropometric type of the head. (2) Methods: The study was conducted on 75 hemifaces of adult formalized cadavers. Ahead of anatomical dissection, each head was measured to establish the anthropometric type, according to Franco and colleagues...

The two subtypes of cannabinoid receptors (CBR), namely CB1 R and CB2 R, belong to the G protein-coupled receptor (GPCR) superfamily and are confirmed as potential therapeutic targets for a variety of diseases such as inflammation, neuropathic pain, and immune-related disorders. Since CB1 R is mainly distributed in the central nervous system (CNS), it could produce severe psychiatric adverse reactions and addiction. In contrast, CB2 R are predominantly distributed in the peripheral immune system with minimal CNS-related side effects...

Cannabinoid CB2 R agonists have gained considerable attention as potential novel therapies for psychiatric disorders due to their non-psychoactive nature, in contrast to CB1 R agonists. In this study, we employed molecular docking to design and synthesize 23 derivatives of cannabidiol (CBD) with the aim of discovering potent CB2 R agonists rather than CB2 R antagonists or inverse agonists. Structure-activity relationship (SAR) investigations highlighted the critical importance of the amide group at the C-3' site and the cycloalkyl group at the C-4' site for CB2 R activation...

The rapid structural evolution and emergence of novel synthetic cannabinoid receptor agonists (SCRAs) in the recreational market remains a key public health concern. Despite representing one of the largest classes of new psychoactive substances, pharmacological data on new SCRAs is limited, particularly at the cannabinoid CB2 receptor (CB2 ). Hence, the current study aimed to characterize the molecular pharmacology of a structurally diverse panel of SCRAs at CB2 , including 4-cyano MPP-BUT7AICA, 4F-MDMB-BUTINACA, AMB-FUBINACA, JWH-018, MDMB-4en-PINACA, and XLR-11...

Cannabinoid CB2 receptor (CB2 R) is a class A G protein-coupled receptor (GPCR) involved in a broad spectrum of physiological processes and pathological conditions. For that reason, targeting CB2 R might provide therapeutic opportunities in neurodegenerative disorders, neuropathic pain, inflammatory diseases, and cancer. The main components from Cannabis sativa, such as Δ9 -tetrahydrocannabinol (Δ9 -THC) and cannabidiol (CBD), have been therapeutically exploited and synthetically-derived analogs have been generated...

With the increased popularity and societal acceptance of marijuana and cannabidiol (CBD) use in humans, there is an interest in using cannabinoids in veterinary medicine. There have been a few placebo-controlled clinical trials in dogs suggesting that cannabis-containing extracts are beneficial for dogs with inflammatory diseases such as osteoarthritis, and there is growing interest in their immunosuppressive potential for the treatment of immune-mediated diseases. Since cannabinoids exhibit anti-inflammatory and immunosuppressive effects in many species, the purpose of these studies was to examine whether the plant-derived cannabinoids, CBD and Δ9 -tetrahydrocannabinol (THC), would also suppress immune function in canine peripheral blood mononuclear cells (PBMCs)...

Terpenes are the most extensive and varied group of naturally occurring compounds mostly found in plants, including cannabis, and have an array of potential therapeutic benefits for pathological conditions. The endocannabinoid system can potently modulate anxiety in humans, rodents, and zebrafish. The 'entourage effect' suggests terpenes may target cannabinoid CB1 and CB2 receptors, among others, but this requires further investigation. In this study we first tested for anxiety-altering effects of the predominant 'Super-Class' terpenes, bisabolol (0...

(1) Background: Twisted carotid bifurcations (CBs) lead to lateralized external carotid arteries (ECAs). Such variants are usually reported on a case-by-case basis. We aimed to study the anatomical possibilities of the axial spin of CB. (2) Methods: Determinations were made bilaterally on a retrospectively assessed sample of 150 cases, 88 males and 62 females. The following types of the axial spin of the CB were determined: type CK1-CB in the coronal plane, with ICA lateral of ECA; type CK3-CB in the coronal plane, with ECA lateral of ICA; the oblique type OK1, with the ECA antero-medial of ICA; the oblique type OK3a, with the ICA antero-medially; the oblique type OK3b, with the ICA postero-laterally; the sagittal type SK2a, with ECA anterior of ICA...

Sepsis is a severe condition secondary to dysregulated host response to infection leading to tissue damage and organ dysfunction. Cannabinoid CB2 receptor has modulatory effects on the immune response. Therefore, this study investigated the effects of a cannabinoid CB2 receptor agonist on the local and systemic inflammatory process associated with pneumonia-induced sepsis. Pneumonia-induced sepsis was induced in mice by intratracheal inoculation of Klebsiella pneumoniae. Tissue and bronchoalveolar lavage (BAL) were collected 6, 24, or 48 h after surgery...

The cannabinoid receptors CB1 and CB2 are class A G protein-coupled receptors (GPCRs) that are activated via endogenous lipids called endocannabinoids. The endocannabinoid system (ECS) plays a critical role in the regulation of several physiological states and a wide range of diseases. In recent years, drug discovery approaches targeting the cannabinoid type 2 receptor (CB2 R) have gained prominence. Particular attention has been given to selective agonists targeting the CB2 receptors to circumvent the neuropsychotropic side effects associated with CB1 receptors...

Multiple Sclerosis (MS) is a prevalent inflammatory disease in which the immune system plays an essential role in the damage, inflammation, and demyelination of central nervous system neurons (CNS). The cannabinoid receptor type 2 (CB2 ) agonists possess anti-inflammatory effects against noxious stimuli and elevate the neuronal survival rate. We attempted to analyze the protective impact of low doses of β-Caryophyllene (BCP) in experimental autoimmune encephalomyelitis (EAE) mice as a chronic MS model...

The discovery of selective agonists of cannabinoid receptor 2 (CB2 ) is strongly pursued to successfully tuning endocannabinoid signaling for therapeutic purposes. However, the design of selective CB2 agonists is still challenging because of the high homology with the cannabinoid receptor 1 (CB1 ) and for the yet unclear molecular basis of the agonist/antagonist switch. Here, the 1,3-benzoxazine scaffold is presented as a versatile chemotype for the design of CB2 agonists from which 25 derivatives were synthesized...

Diabetic nephropathy (DN) is a condition that leads to end-stage chronic kidney disease characterized by inflammation and a deficiency of nitric oxide (NO). Cannabinoid receptor (CB2 ) activation by specific agonist reduces nuclear factor kappa beta (NF-κβ) expression. Beta caryophyllene (BCP), a natural CB2 receptor activator, protects kidney function in several diseases. L-Arginine (LA) modulates several physiological processes by donating nitric oxide (NO). Hence, we tested a novel BCP-LA combination to treat DN and investigated its molecular mechanisms...

Cannabis use during pregnancy is increasing in the last few years potentially because of decreased perception of the risk of harm. Regardless, recent evidence demonstrated that prenatal cannabis exposure is associated with adverse outcomes. To date there is limited evidence of the impact of cannabis exposure during pregnancy on the reproductive health of the offspring. The biological effects of cannabis are mediated by two cannabinoid receptors, CB1 and CB2 . We previously demonstrated that CB2 is highly expressed in mouse male and female fetal germ cells...