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Readable research linked to original sources
Browse normalized, publication-ready research with direct links to its evidence and source.
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Readable research linked to original sources
Browse normalized, publication-ready research with direct links to its evidence and source.
40 articles
Newest firstSynthetic cannabinoid receptor agonists constitute a prominent class of new psychoactive substances (NPS), in which minor structural modifications can markedly influence in vivo pharmacological outcomes. In this study, methoxy-substituted derivatives of JWH-018 were synthesized to examine the effect of substitution position on behavioral activity. JWH-018-5-OMe and JWH-018-6-OMe were evaluated using four in vivo a…
Open article record in new tab ↗Opioid use disorder (OUD) remains a major public health crisis, underscoring the urgent need for safer and more effective treatments. Cannabinoid CB2 receptor (CB2R) agonists show therapeutic promise for neuropsychiatric disorders and pain, with minimal psychoactive effects by themselves, but their potential in treating OUD is not well defined. Here, we report that MRI-2594, a novel, highly selective CB2R agonist,…
Given the increasing availability of high-potency Δ9-tetrahydrocannabinol (Δ9-THC) products, understanding potency-related effects of Δ9-THC on driving performance is an important public safety issue. This randomized, double-blind, placebo-controlled, within-subjects trial examined the effects of smoked cannabis with varying Δ9-THC concentrations on simulated driving. Adults aged 19–45 who regularly used cannabis…
Prescription opioid misuse is a significant public health concern among individuals with chronic pain. Treating severe pain often requires high doses of opioids, increasing the risk of developing an opioid use disorder. Cannabidiol (CBD) is a non-intoxicating component of cannabis that has shown therapeutic potential without abuse liability. This study investigated the effects of CBD on oxycodone self-administrati…
Endocannabinoids (eCBs) are lipid-derived neuromodulators that regulate numerous neurophysiological processes by modulating synaptic transmission. Synthesised on demand in response to increased postsynaptic intracellular calcium or activation of postsynaptic G-protein coupled receptors, eCBs are rapidly degraded, resulting in transient, tightly regulated signalling. Dysregulation in the endocannabinoid system (ECS…
Gut-brain signaling influences alcohol consumption and addiction behaviors. We found that selectively deleting cannabinoid receptor 1 (CB1R) from advillin+ peripheral sensory neurons eliminates the inhibitory effect of the peripheral CB1R antagonist JD5037 on voluntary ethanol intake (VEI). Similar results were seen in mice with CB1R deletion in Phox2b+ nodose ganglia (NGA), but not in Wnt+ dorsal root ganglia. Th…
Cannabidiol (CBD) is widely perceived as a safe and effective treatment for a growing list of health indications and use for general wellness. Evidence for its safety and efficacy comes from a variety of sources, including preclinical studies, clinical trials, and observational studies of real-world evidence. The challenge in interpreting these data is that CBD products are diverse with respect to format, formulat…
Open article record in new tab ↗Cisplatin (CDDP) is an effective chemotherapeutic agent used to treat solid tumors, but it can cause irreversible hearing loss. Currently, there are no specific preventive measures available for this side effect. G protein-coupled receptor 55 (GPR55) exhibits antioxidant, anti-inflammatory, and anti-apoptotic properties and is implicated in various disease processes. Nevertheless, whether GPR55 plays a role in CDD…
Open article record in new tab ↗The chikungunya virus (CHIKV) outbreak imposes a significant burden on healthcare systems and raises an urgent need for effective antiviral therapies. So far there are no specific drugs against CHIKV. A CHIKV macrodomain is critical for virulence and counteracts the host immune response, representing a promising antiviral drug target. Here, we describe small molecule inhibitors targeting the CHIKV macrodomain. Com…
Drug development for developmental and epileptic encephalopathies (DEEs) follows different strategies on one hand including disease-targeting precision medicine approaches considering the genetic variants and pathomechanisms in DEEs and on the other hand including therapeutic approaches with novel targets or second-generation drug candidates that may be of interest beyond selected DEEs. Although the first group of…
Open article record in new tab ↗Although alcohol use disorder (AUD) is highly prevalent, only a few medications are approved for its treatment leaving much room for improvement. Cannabidiol (CBD) might be a particularly promising candidate, with preclinical data suggesting that CBD is effective in targeting AUD symptoms and disease processes that drive alcohol use and relapse, due to its anti-craving, stress-reducing, and anti-compulsive effects…
Regulatory T cells (Tregs) have multiple roles in the tumor microenvironment (TME), which maintain a balance between autoimmunity and immunosuppression. This research aimed to investigate the interaction between cancer stemness and Regulatory T cells (Tregs) in the breast cancer tumor immune microenvironment. Breast cancer stemness was calculated using one-class logistic regression. Twelve main cell clusters were…
Safe and effective pain management is a critical healthcare and societal need. The potential for acute liver injury from paracetamol (ApAP) overdose; nephrotoxicity and gastrointestinal damage from chronic non-steroidal anti-inflammatory drug (NSAID) use; and opioids' addiction are unresolved challenges. We developed SRP-001, a non-opioid and non-hepatotoxic small molecule that, unlike ApAP, does not produce the h…
Pharmacological treatment of psychiatric disorders remains challenging in clinical, pharmacological, and scientific practice. Even if many different substances are established for treating different psychiatric conditions, subgroups of patients show only small or no response to the treatment. The neuroinflammatory hypothesis of the genesis of psychiatric disorders might explain underlying mechanisms in these non-r…
Very recently, we have developed a new generation of ligands targeting the cannabinoid receptor type 2 (CB2R), namely JR compounds, which combine the pharmacophoric portion of the CB2R positive allosteric modulator (PAM), EC21a, with that of the CB2R selective orthosteric agonist LV62, both synthesized in our laboratories. The functional examination enabled us to identify JR14a, JR22a, and JR64a as the most promis…
Cannabidiol (CBD) is thought to have multiple biological effects, including the ability to attenuate inflammatory processes. Cannabigerols (CBGA and its decarboxylated CBG molecule) have pharmacological profiles similar to CBD. The endocannabinoid system has recently emerged to contribute to kidney disease, however, the therapeutic properties of cannabinoids in kidney disease remain largely unknown. In this study,…
Open article record in new tab ↗The discovery of natural drug metabolites is a leading contributor to fulfilling the sustainable development goal of finding solutions to global health challenges. Depsidones are a class of polyketides that have been separated from lichens, fungi, sponges, and plants and possess various bioactivities, including cytotoxic, antimicrobial, antimalarial, antituberculosis, acetylcholinesterase and α-glucosidase inhibit…
The identification of new modulators for Cannabinoid Receptors (CBRs) has garnered significant attention in drug discovery over recent years, owing to their manifold pathophysiological implications. In the context of hit identification, the availability of robust and sensitive high-throughput screening assays is essential to enhance the likelihood of success. In this study, we present the development and validatio…
Open article record in new tab ↗(-)-Cannabidiol (CBD) and (-)-cannabigerol (CBG) are two major non-psychotropic phytocannabinoids that have many beneficial biological properties. However, due to their low water solubility and prominent first-pass metabolism, their oral bioavailability is moderate, which is unfavorable for medicinal use. Therefore, there is a great need for appropriate chemical modifications to improve their physicochemical and b…
The emergence of a novel coronavirus that later on rendered a global pandemic, caused desperation within the communities and drove increased interest in exploring medicinal plant-based therapeutics to treat and prevent severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virus infections. Many medicinal plants have been reported to have antiviral, anti-inflammatory, and immunomodulatory effects that hinder…