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Together these results establish GPR55 as an additional cannabinoid receptor that activates signaling pathways distinct from CB1 or CB2, and that may increase neuronal excitability and have additional effects through its action on RhoA.
The expression of GPR55 in brain areas known to govern energy household and functions as well as in enteric epithelial cells and enteric neurons suggests that GPR55 is likely involved in GI processes such as motility and possibly secretion.
Physiological function GPR55 is widely expressed in the brain, especially in the cerebellum. It is expressed in the jejunum and ileum but apparently not more generally in the periphery. Osteoblasts and osteoclasts express GPR55 and this has been shown to regulate bone cell function.
CB1 and CB2 cannabinoid receptors are the primary targets of endogenous cannabinoids (endocannabinoids). These G protein-coupled receptors play an important role in many processes, including metabolic regulation, craving, pain, anxiety, bone growth, and immune function.
PSB-SB-487 is a potent GPR55 antagonist and CB2 agonist with an IC50 value of 0.113 M for GPR55, and a Ki value of 0.292 M for human CB2. PSB-SB-487 can be used for researching diabetes, Parkinsons disease, neuropathic pain, and cancer.
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