Cannabinoidi

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].

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.

Heptadecanoyl ethanolamide, an endogenous cannabinoid, serves as a synthetic analog of PEA, featuring an odd-numbered (17-carbon) fatty acid chain [1].

Tedalinab is an effective and selective cannabinoid receptor 2 agonist.

Tricosanoyl ethanolamide, a fatty N-acyl ethanolamine within the endocannabinoid family, has an ethanolamine metabolite whose significance remains to be established.

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

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

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

γ-Linolenoyl monoethanolamide, a fatty N-acyl ethanolamine, acts as an endocannabinoid [1] [2].

PF-03550096, an orally active synthetic cannabinoid (CB), selectively binds to peripheral CB2 receptors with a Ki value of 7.9 nM, demonstrating analgesic activity [1].

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo.

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

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

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

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

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>GP 1a: potent CB2 receptor agonist (EC50=7.1), 30x CB2 over CB1 preference, boosts P-ERK1/2, aids skin healing, anti-inflammatory.</p>

<p>GW 833972A: selective CB2 agonist; reduces neural depolarization and citric acid cough in animals.</p>

<p>Cannabichromevarin is a phytocannabinoid naturally found in very low levels compared to other cannabinoids from which it differs in having a propyl chain in place of a pentyl chain1. Based on its structure, it is believed to act as a potent anandamine inhibitor similarly to cannabichromene, however, the majority of its pharmacological and toxicological properties are currently unknown. In vitro assays have shown cannabichromevarin protect against oxidative stress in vitro in macrophages2. It was recently shown to be effective for treatment-resistant epilepsy in a patented combination with cannabidiol in a recent open-ended clinical trial3.</p>