CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

Hexyl resorcinol derivative 29 is a CB2 selective competitive antagonist/reverse agonist demonstrating notable potency. Meanwhile, Olivanol and 5-(2-methyloctane-2-yl) resorcinol derivatives 23 and 24 exhibit substantial antinociceptive effects. Notably, compound 24 activates both cannabinoid and TRPV1 receptors.

GP 2A is a selective agonist of CB2 receptor.

CB2 PET Radioligand 1 (compound [18F]9) is a positron emission tomography (PET) radioligand with high affinity for the human cannabinoid receptor 2 (hCB2, Ki=7.7 nM). It is synthesized via Cu-mediated 18F-fluorination and demonstrates significant brain uptake in a mouse model of neuroinflammation [1].

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-2 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 has studies research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

CB29 is a specific inhibitor of aldehyde dehydrogenase 3A1 (ALDH3A1).

β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.

Cannabigerol is a high affinity α±2-adrenergic receptor agonist, moderate affinity 5-HT1A receptor antagonist, and low affinity CB1 receptor antagonist ; also binds to the CB2 receptor; it can relieve interocular pressure, which may be of benefit in the treatment of glaucoma.

CB2R agonist 2 (cis-17-para) is a CB2R agonist [1].

CB2R Probe 1, a cannabinoid 2 receptor (CB2R) fluorescent probe, exhibits both safety and environmental friendliness, boasting a dissociation constant (K i) of 130 nM. Notably, it demonstrates low cytotoxicity within cancer cells [1].

ICCB280 was capable of inducing differentiation and apoptosis of ATRA-resistant patient blasts strongly signify that the activity of this compound can overcome resistance to other current therapies for AML with an unfavorable prognosis.

CB2R/FAAH modulator-3 (compound 27) is a modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-3 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 has research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].

Hemopressin (rat) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB2 cannabinoid receptors. Hemopressin exerts antinocicep

GW 833972A is a selective CB2 receptor agonist.GW 833972A has an inhibitory effect on induced neural depolarization and on citric acid-induced cough in an animal model.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

RVD-Hpα acetate is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

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

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

CB2R PAM is an orally active cannabinoid type 2 receptor (CB2Rs) positive mutational modulator that enhances CP 55940 and 2-Arachidonylglycerol-stimulated [35S]GTPγS binding to CB2 receptors, but has no effect in the absence of agonists. ...CB2R PAM shows anti-injury activity in a mouse model of neuropathic pain.

CB2R agonist 1, a selective ligand for the cannabinoid receptor subtype 2 (CB2R), demonstrates a high affinity and excellent selectivity, with an EC50 value of 0.56 µM, favoring human CB2R over CB1R. It plays an immunomodulatory role by regulating the production of both pro-inflammatory and anti-inflammatory cytokines.

KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and CLK4 , with an IC 50 of 16.5 nM for CLK1 . KH-CB20 also can inhibits DYRK1A ( IC 50 =57.8 nM) and CLK3 ( IC 50 =488 nM).

CB2R-IN-3 is a selective antagonist of cannabinoid type 2 receptor (CB2R) . CB2R-IN-3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R-IN-3 can be combined with CB65 , the activator of CB2R. CB2R-IN-3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines [1] .

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. Also high affinity CB2 positive allosteric modulator (Ki = 50 nM).

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor with a Ki of 2.4 μM.

N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. The different types of NAE can be derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-arachidonoyl ethanolamine is the precursor of arachidonoyl ethanolamide (AEA), also known as anandamide. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM, compared to 46 nM for δ9-THC.

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

EHP-101 (VCE-004.8) is a specific dual agonist of PPARγ and CB2 receptor with potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

(±)10(11)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 0.43 and 22.5 nM for CB1 and CB2 receptors, respectively). It is produced though direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. 10,11-EDP epoxide (12.5 and 25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It induces apoptosis and inhibits cell migration in a wound-healing assay in 143B, MG63, and HOS osteosarcoma cells. (±)10(11)-EDP ethanolamide also reduces tube formation by human umbilical vein endothelial cells (HUVECs) in a Matrigel assay.

N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. For example, arachidonoyl ethanolamide (AEA) is an endogenous neurotransmitter that evokes cellular responses by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). The different types of NAE are derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-palmitoyl ethanolamine (GP-NPEA) is the metabolic precursor of palmitoyl ethanolamide (PEA). PEA is an endogenous cannabinoid found in brain, liver, and other mammalian tissues, that has potent anti-inflammatory activity in vivo. PEA has low affinity for peripheral cannabinoid (CB2) and no appreciable affinity for central cannabinoid (CB1), suggesting that its efficacy is through a different receptor.

Bone mass and shape is continuously remodeled by the concerted and balanced action of osteoblasts (bone forming cells) and osteoclasts (bone-resorbing cells). The endocannabinoid system plays an essential role in the maintenance of normal bone mass via signaling through the CB2 receptor. N-Oleoyl-L-serine is an endogenous lipid that has been reported to stimulate bone formation and to inhibit bone resorption.

JWH 302, a cannabimimetic indole, exhibits 5-fold selectivity for the central cannabinoid (CB1) receptor, evidenced by a Ki value of 17 nM, versus the peripheral cannabinoid (CB2) receptor, which has a Ki value of 89 nM. Additionally, JWH 302 stimulates GTPγS binding of CB1 and CB2 receptors with EC50 values of 29.3 nM and 24.4 nM, respectively.

Noladin ether is a selective cannabinoid CB1 receptor agonist (Ki=21.2 nM). Noladin ether can cause hypothermia, intestinal immobility, and mild pain relief.

JWH 182, a potent synthetic cannabinoid (CB) can activate the central CB1 receptor and the peripheral CB2 receptor with a Ki value of 0.65 nM and 1.1 nM, respectively. Its effects in cells and animals have not evaluated.

JWH 072 , known as synthetic cannabinoid (CB), displays a higher affinity to the peripheral CB2 receptor (Ki = 170 nM) than the central CB1 receptor (Ki = 1,050 nM). Its physiological and toxicological properties are still on study.

O-2050 is a high affinity cannabinoid CB 1 receptor antagonist with a K i of 2.5 nM. O-2050 inhibits cannabinoid CB 2 receptor with Ki of 0.2 nM. O-2050 decreased food intake in mice and caused locomotor stimulation in mice [1].

N-Acetylpurinomycin is a selective agonist of CB2 receptor.

JWH 081, a cannabimimetic aminoalkylindole, has a high-affinity to the central cannabinoid (CB1) receptor (Ki =1.2 nM) and ten-fold reduced affinity to the peripheral cannabinoid (CB2) receptor (Ki = 12.4 nM). JWH 081-N-(cyclohexylmethyl) analog is a synt

CB1/2 agonist 4 (compound 24) is a CB1 full agonist (EC50: 15.09 nM) and a CB2 partial agonist (EC50: 1.16 nM). CB1/2 agonist 4 has significant anti-harm-sensing activity and also activates cannabinoid and TRPV1 receptors (IC50: 0.8 μM, EC50: 0.12 μM). , EC50: 0.12 μM).

L-759,656 is highly selective CB2 receptor agonist (CB1 Ki = 4888 nM, CB2 Ki = 11.8 nM). L-759,656 potently inhibits forskolin-stimulated cAMP production in CHO cells (EC50 = 3.1 nM).

Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.

JWH 249 is a synthetic cannabinoid. It potently activates the central CB1 and peripheral CB2 receptors (Ki: 8.4 and 20 nM, respectively).