cb2 receptor modulator  (Pfizer Inc)

Journal: PLoS ONE

Article Title: Cannabinoid Receptors Are Overexpressed in CLL but of Limited Potential for Therapeutic Exploitation

doi: 10.1371/journal.pone.0156693

Figure Lengend Snippet: B-cell enriched primary cells of 7 CLL patients (97.7% ± 1.04 CD19+CD5+) were incubated in transwell plates for 4h before the number of migrated cells was determined. Control experiments included CXCL12 alone (control), no CXCL12 (control w/o CXCL12), incubation with vehicle (DMSO, ethanol), and incubation with the CXCR4 inhibitor AMD3100. CLL cells were incubated either with agonist (ACEA, JWH133), antagonist (AM251, AM630), or a combination of antagonist plus agonist before migration (CB1: AMS251&ACEA; CB2: AM630&JWH133). Bars represent the mean values of migration indices + standard deviations, hatched lines indicate experimental blocks. *p = 0.0006; **p<0.0001.

Article Snippet: Cannabinoids used in cytotoxicity and migration experiments were ACEA (CB1 agonist), AM251 (CB1 antagonist, μ-opioid receptor antagonist, GPR55 agonist, ion channel activation), AM630 (CB2 antagonist/inverse agonist, weak partial CB1 agonist, ion channel activation), (-)-cannabidiol (CNB) (GPR55 & weak CB1 antagonist, CB2 inverse agonist, weak agonist at VR1 vanilloid receptors, and modulator at opioid receptors), JWH133 (CB2 antagonist), and R-(+)-methanandamide (RM) (CB1 agonist, activity against GPR and ion channels) purchased from TOCRIS Bioscience (Bristol, UK).

Techniques: Incubation, Control, Migration