Introduction: β-carbolines are shown to have significant anti-inflammatory effect via the inhibition of some inflammatory mediators including TNF-α and PGE2. In previous studies Purkinje cell deterioration have been proposed the dominant pathogenesis of harmaline toxicity. WIN55, 212-2 is a non-selective cannabinoid CB1 and CB2 receptor agonist. Combination of WIN55, 212-2 ...

An agonist that acts through a single receptor can activate numerous signaling pathways. Recent studies have suggested that different ligands can differentially activate these pathways by stabilizing a limited range of receptor conformations, which in turn preferentially drive different downstream signaling cascades. This concept, termed "biased signaling" represents an exciting therapeutic opp...

Osteoarthritis (OA) of the joint is a prevalent disease accompanied by chronic, debilitating pain. Recent clinical evidence has demonstrated that central sensitization contributes to OA pain. An improved understanding of how OA joint pathology impacts upon the central processing of pain is crucial for the identification of novel analgesic targets/new therapeutic strategies. Inhibitory cannabino...

Cannabinoids suppress neuropathic pain through activation of cannabinoid CB1 and/or CB2 receptors; however, unwanted CB1-mediated cannabimimetic effects limit clinical use. We asked whether CP55,940 [(-)-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-4-(3-hydroxypropyl)cyclohexanol], a potent cannabinoid that binds with similar affinity to CB1 and CB2 in vitro, produces functionally separable CB1- ...

There are two well-characterised isoforms of cannabinoid receptor; CB1 and CB2 and of these CB2 is under active investigation as a potential target for treatment of the chronic pain associated with widespread and intractable joint diseases osteoarthritis and rheumatoid arthritis. The recent report by Fukuda et al (BMC Musculoskelet Disord15:275, 2014) in BMC Musculoskeletal Disorders investigat...

Cannabinoids are known to interact with CB1 and CB2 receptors expressed in the nervous and immune system, respectively, and mediate a wide range of effects, including anti-inflammatory properties. However, cannabinoids that bind CB1 are also psychoactive thereby limiting their clinical use. In this study, we investigated the immunosuppressive properties of JWH-015, a synthetic CB2-selective ago...

Mammalian tissues express at least two types of cannabinoid receptor, CB1 and CB2, both G protein coupled. CB1 receptors are expressed predominantly at nerve terminals where they mediate inhibition of transmitter release. CB2 receptors are found mainly on immune cells, one of their roles being to modulate cytokine release. Endogenous ligands for these receptors (endocannabinoids) also exist. Th...

Cannabinoid receptor 2 agonists and inverse agonists are emerging as new therapeutic options for a spectrum of autoimmune-related disease. Of particular interest, is the ability of CB2 ligands to regulate microglia function in neurodegenerative diseases and traumatic brain injury. We have previously reported the receptor affinity of 3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-phenyl-methanone (...

introduction: β-carbolines are shown to have significant anti-inflammatory effect via the inhibition of some inflammatory mediators including tnf-α and pge2. in previous studies purkinje cell deterioration have been proposed the dominant pathogenesis of harmaline toxicity. win55, 212-2 is a non-selective cannabinoid cb1 and cb2 receptor agonist. combination of win55, 212-2 and am 251(cb1-select...

The cannabinoid type two receptors (CB2), an important component of the endocannabinoid system, have recently emerged as neuromodulators and therapeutic targets for neurodegenerative diseases including Parkinson's disease (PD). The downregulation of CB2 receptors has been reported in the brains of PD patients. Therefore, both the activation and the upregulation of the CB2 receptors are believed...