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GeneBLAzer® CNR1-Gα15-NFAT-bla CHO-K1 cells contain the human Cannabinoid Receptor 1 (CNR1) stably integrated into the GeneBLAzer® Gα15-NFAT-bla CHO-K1 cell line. GeneBLAzer® Gα15-NFAT-bla CHO-K1 cells (Cat. no. K1537) contain a beta-lactamase reporter gene under control of the Nuclear Factor of Activated T-cells (NFAT) response element and the Promiscuous G protein, Gα15.
The GeneBLAzer® CNR1-Gα15-NFAT-bla CHO-K1 cells are functionally validated for Z' and EC50 concentrations of CP-55,940. In addition, GeneBLAzer® CNR1-Gα15-NFAT-bla CHO-K1 cells have been tested for assay performance under variable conditions. These data are found in the Validation & Assay Performance Summary.
The cannabinoid receptors are a family of GPCRs named after their endogenous ligand Delta9-tetrahydrocannabinol (Delta9-THC). Delta9-THC is the psychoactive component of Cannabis sativa (marijuana). CNR1 is present in many tissues throughout the body. The highest concentrations of cannabinoid receptors are in the neurons of the brain, the hippocampus, cerebral cortex, basal ganglia, and the cerebellum. Low-level expression occurs in the lung, testis, and uterus, as well as vascular tissue. Delta9-THC and CP55,940 are endogenous agonists of the CNR1 pathway. Several Delta9-THC and CP55,940 analogs have been synthesized, including HU 210 and WIN 55,212-2. The CNR1 and CNR2 receptors have equal affinity for cannabinoid agonists, but several antagonists that are subtype selective have been synthesized. Examples of these antagonists are AM251, LY-320135, and SR 141716A.