Cannabinoids

GSK494581A is a GPR55 agonist and glycine transporter subtype 1 inhibitor.

<p>URB447, a peripherally restricted CB1 cannabinoid antagonist with IC50 values of 313 nM for rat CB1 receptor and 41 nM for human CB2 receptor, effectively reduces food intake and body weight gain in mice. It achieves these effects without penetrating the brain or antagonizing central CB1-dependent responses, making it a potential research tool for obesity studies [1].</p>

<p>CB-52 acts as a neutral antagonist and ligand for the CB2 cannabinoid receptor [1].</p>

<p>Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester functioning as a central cannabinoid receptor (CB1) antagonist and exhibits</p>

<p>O-Arachidonoyl glycidol (compound 1), a 2-arachidonoylglycerol (2-AG) analog, effectively inhibits the hydrolysis of cytosolic 2-oleoylglycerol (2-OG) with an IC50 value of 4.5 µM, and also blocks 2-OG and anandamide hydrolysis in membrane fractions with IC50 values of 19 µM and 12 µM, respectively [1].</p>

<p>OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).</p>

<p>AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor.</p>

<p>CB-25 is a partial agonist ligand of CB1 cannabinoid receptors, augmenting Forskolin-induced cAMP formation in cancer cells, though not affecting hCB1-CHO cells</p>

<p>CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.</p>

O-2050: strong CB1 antagonist (Ki 2.5 nM), CB2 inhibitor (Ki 0.2 nM); reduces mouse food intake, increases activity.

<p>GW405833 hydrochloride, a potent and selective agonist of the cannabinoid-2 (CB2) receptor (EC 50 = 0.65 nM; maximum inhibition = 44.6%), exhibits significant antihyperalgesic effects in various rodent pain models [1] [2] [3].</p>

<p>Tedalinab is an effective and selective cannabinoid receptor 2 agonist.</p>

<p>2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an "entourage" effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.</p>

<p>CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and</p>

<p>MRL-650 is an oral, selective CB1 agonist; IC50: CB1=7.5 nM, CB2=4100 nM; anorexigenic effects noted.</p>

<p>(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].</p>

<p>Amauromine is a peripherally selective and potent cannabinoid receptor type 1 (CB1) receptor antagonist, a novel alkaloid with vasodilatory activity.</p>

<p>CB 65 is a high affinity and selective CB2 receptor agonist with Ki values of 3.3 and &gt; 1000 nM for CB2 and CB1 receptors respectively.</p>

<p>GSK-554418A, a novel azaindole CB(2) agonists, is used for the treatment of chronic pain. It is efficacious in the acute model and the chronic joint pain model.</p>

<p>Hemopressin(rat) TFA, a nonapeptide from hemoglobin α1-chain, selectively inhibits CB1 receptors and reduces inflammatory pain.</p>