Cannabinoids

<p>Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.</p>

<p>MDMB-FUBICA is a potent agonist of the cannabinoid receptors and exhibits psychoactive properties. It can be utilized in e-cigarettes.</p>

<p>HU-308, a synthetic cannabinoid analogue, is a highly selective agonist of the CB2 receptor. It demonstrates an affinity for the CB2 receptor that is over 440 times greater than its affinity for the CB1 receptor, which are predominantly found in immune cells. This compound plays a crucial role in modulating the immunosuppressive effects of the endocannabinoid system (ECS). Additionally, HU-308 possesses anti-inflammatory and neuroprotective properties, and it regulates the function of microglia. Its potential applications include research into neuroinflammation and retinal diseases.</p>

<p>CB1 antagonist 4 is an inverse agonist of cannabinoid receptor 1 (CB1) with an IC50 of 0.4 nM. It can reduce body weight, improve plasma inflammatory markers, and enhance glucose homeostasis [1].</p>

<p>GAT564, an allosteric CB1R modulator, shows EC50s of 87 nM (cAMP) &amp; 320 nM (β-arrestin2) and lowers IOP effectively in glaucoma mice.</p>

<p>MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2), demonstrating an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. The compound exhibits good affinity for CB2 receptors, with Ki values of 422 nM for humans and 238 nM for rats. In rat models, MDA7 shows analgesic activity.</p>

<p>HU 433, a synthetic cannabinoid, acts as a CB2 receptor agonist and is an enantiomer of HU 308. It provides anti-inflammatory and neuroprotective effects by binding to the CB2 receptor, primarily found on immune cells, thereby modulating immune responses and inflammation. Additionally, HU 433 influences microglial signaling pathways, particularly LPS and IFNγ-mediated routes, affecting the phosphorylation of MAPKs, including ERK1/2, JNK, p38, and Akt. This compound is valuable in researching neuroinflammation and retinal diseases.</p>

<p>Bzo-poxizid is a synthetic cannabinoid and a psychoactive substance.</p>

<p>CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.</p>

<p>BNS808 is an orally active, selective CB1R antagonist with an IC50 of 0.8 nM, demonstrating significant selectivity for CB2R and minimal brain penetration. It is being studied for the treatment of obesity and related metabolic complications, such as metabolic dysfunction-associated steatotic liver disease (MASLD). BNS808 reduces drug exposure to the central nervous system, enhancing safety, and minimizes drug interactions through high plasma protein binding.</p>

<p>CBR Agonist-2: CB1 receptor agonist, EC50 - 960 nM, Ki - 970 nM, useful for hCB1R-related disease research.</p>

<p>CBR Agonist-1 targets CB1R and CB2R with Ki of 0.18 μM and 1.22 μM, useful for studying cannabinoid-related diseases.</p>

<p>Compound 29 is a potent, CB2-selective antagonist/reverse agonist. Derivatives 23 &amp; 24 offer antinociception; 24 activates cannabinoid/TRPV1 receptors.</p>

<p>(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a potent and selective antagonist of cannabinoid receptor type 1 (CB1R) and inducible nitric oxide synthase (iNOS), with a binding affinity (Ki) of 5.7 nM for CB1R. It holds promise as an investigative tool in liver fibrosis research due to these characteristics.</p>

<p>WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.</p>

<p>AM-2232 (UNII-40KCH8YIKP) is a potent and unselective agonist of the cannabinoid receptors.</p>

<p>In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand</p>

<p>AEF0117 is a signaling inhibitor of CB1-SSi that inhibits cannabinoid self-administration and can be used to study cannabis withdrawal.</p>