cb2r antagonist sr144528  (MedChemExpress)

Journal: International Journal of Molecular Sciences

Article Title: CBD Versus CBDP: Comparing In Vitro Receptor-Binding Activities

doi: 10.3390/ijms25147724

Figure Lengend Snippet: Comparative analysis of ( a ) CB1 and ( b ) CB2 antagonists (AM251, SR144528) and cannabinoids (CBD, CBDP) on cAMP activity following (±)-CP55,940 stimulation using a DiscoverX HitHunter cAMP XS+ assay. One hundred percent relative activity was normalized to maximum activity of AM251 (CB1) and SR144528 (CB2); 0% relative activity was normalized to response of vehicle control. **** p < 0.0001, ** p < 0.01, * p < 0.05 versus vehicle control. #### p < 0.0001 versus CBDP. Error bars represent the standard deviation of three independent measurements.

Article Snippet: Naturally occurring enantiomers of CBD and CBDP ((−)-CBD and (−)-CBDP) were purchased as pure analytical standards (in acetonitrile) from Cayman Chemicals. (±)-CP55,940, AM251, SR144528, serotonin, dopamine, naloxone hydrochloride, and enkephalin were provided by Eurofins.

Techniques: Activity Assay, Control, Standard Deviation

Journal: The Journal of Clinical Investigation

Article Title: Type 2 cannabinoid receptor expression on microglial cells regulates neuroinflammation during graft-versus-host disease

doi: 10.1172/JCI175205

Figure Lengend Snippet: ( A ) Chemical structure of SMM-189. ( B and C ) Serum level ( B ) and brain concentration ( C ) of SMM-189 in naïve and Balb/c mice transplanted with B6 BM or B6 BM and spleen cells. ( D ) Ratio of brain to serum SR144528 and SMM-189 concentrations. Results in B – D are from 2 experiments ( n = 5–10 mice/group). ( E ) 2-AG levels in the amygdala, brainstem, cerebellum, and prefrontal cortex 14 days after transplantation. Results are from 3 experiments ( n = 14–15 mice/group). ( F – N ) Balb/c recipients were transplanted with B6 BM alone or B6 BM and spleen cells. Animals were then treated with SMM-189 or vehicle control. ( F ) The percentage and absolute number of donor CD4 + and CD8 + T cells in the brains of mice 14 days after transplantation. ( G – J ) The absolute number of CD4 + and CD8 + T cells that produced IFN-γ, TNF-α, IL-6, or GM-CSF. ( K ) Absolute number of microglial cells. ( L and M ) Absolute number of MHC class II, CD80, and CD86 expressing microglial cells. Results in panels F – M are from 2 experiments ( n = 6–10 mice/group). ( N ) Representative Western blot images and scatterplots depicting normalized expression of cleaved caspase 3 in the brain from mice treated with either SMM-189 or a vehicle control. Vertical lines on Western blots denote noncontiguous gel lanes. Data are from 2 experiments ( n = 4–10 mice/group). ( O – Q ) Balb/c recipients were transplanted with B6 BM alone ( n = 6) or with B6 spleen cells ( n = 10) and treated with SMM-189 or vehicle. Overall survival ( O ), serial weight curves ( P ), and clinical score ( Q ) are shown. Results are from 2 experiments ( n = 6–10 mice/group). In panels P and Q , BM alone mice only received vehicle. Data are presented as mean ± SD. Statistics were performed using a 1-way ANOVA with Tukey’s test for multiple group comparisons. * P < 0.05, ** P < 0.01, *** P < 0.001, **** P < 0.0001. Source data are provided as a file.

Article Snippet: SR144528 is a CB2R inverse agonist/antagonist and was purchased from Tocris Bioscience.

Techniques: Concentration Assay, Transplantation Assay, Control, Produced, Expressing, Western Blot