The cannabinoid receptor CNR1 is a G-protein-coupled receptor for endogenous cannabinoids (eCBs) like anandamide (AEA) and 2-arachidonoylglycerol (2-AG), as well as phytocannabinoids like delta9-tetrahydrocannabinol (THC). It mediates diverse cannabinoid-induced effects, influencing processes such as food intake, memory, gastrointestinal motility, pain, anxiety, and ambulatory activity, primarily through cyclic AMP reduction.
In the hypothalamus, CNR1 exhibits dose-dependent effects on mitochondrial respiration, enhancing it at low agonist doses and suppressing it at higher doses via G-protein alpha-i activation. This pathway decreases cyclic AMP, inhibits protein kinase A (PKA)-mediated phosphorylation of mitochondrial electron transport subunits (e.g., NDUFS2), and modulates energy metabolism. It also inhibits leptin-induced reactive oxygen species (ROS) formation and promotes orexigenic beta-endorphin release from POMC neurons, enhancing food intake. In the hippocampus, CNR1 regulates energy production and mediates depolarization-induced suppression of inhibition (DSI), transiently reducing GABAergic and excitatory synaptic transmission.
CNR1 modulates voltage-gated calcium channels in vascular smooth muscle cells and superior cervical ganglions, leading to vasodilation and reduced vascular tone. In adipose tissue, it enhances SREBF1, ACACA, and FASN expression, driving lipid synthesis. In the liver, it promotes lipogenesis and reduces fatty acid oxidation. In macrophages, CNR1 activation triggers a pro-inflammatory response via NLRP3 inflammasome activation, contributing to type-2 diabetes progression and pancreatic beta-cell loss.
| Product Name | Recombinant Human Cannabinoid Receptor 1 (CNR1) Protein (His), Active |
| Accession | P21554 |
| Endotoxin | Less than 1.0 EU/ug as determined by LAL method. |
| Host Species | Human |
| Gene | CNR1 |
| Source | Mammalian cell |
| Protein Expression Range | 1-472aa |
| Tag | C-10His |
| Molecular Mass | 54.6 kDa |
| Form | Lyophilized powder |
| Buffer | Lyophilized from a 0.2 μm filtered PBS, 6% Trehalose, pH 7.4 |
| Storage | 1. Store at -20～C/-80～C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4～C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20～C/-80～C. Protein in lyophilized powder form is stable for up to 12 months at -20～C/-80～C. |
| Bioactivity | Measured by its binding ability in a functional ELISA. Immobilized Human CNR1 at 10 μg/mL can bind Anti-CNR1 recombinant antibody , the EC 50 is 41.72-63.54 ng/mL. |
