CB1 Agonist

GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC₅₀ values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.

Noladin ether is a potent and selective agonist of cannabinoid CB₁ receptor, with a K_i of 21.2 nM. Noladin ether can cause hypothermia, intestinal immobility, and mild antinociception.

CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The K_i values for CB2R/FAAH modulator-3 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 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

Docosatetraenylethanolamide (DEA) is a cannabinoid receptor 1 (CB1) agonist. Docosatetraenylethanolamide inhibits the specific binding of cannabinoid probe to rat synaptosomal membranes with a K_i value of 34.4 nM. Docosatetraenylethanolamide can be used in the research of nervous system.

AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC₅₀s of 45.71 and 0.076 nM, respectively.

(±)5(6)-EET Ethanolamide is a metabolite of Anandamide (HY-10863) generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has K_i values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.

CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating G_i/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain.

BAY 38-7271 is selective and highly potent and cannabinoid CB₁/CB₂ receptor agonist, with K_is of 1.85 nM and 5.96 nM for recombinant human CB₁ receptor and CB₂ receptor, respectively. BAY 38-7271 has strong neuroprotective properties.

MDA7 is the selective agonist for cannabinoid receptor 2 with EC₅₀ of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with K_i of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.

MN-25 (compound 4a) is an orally active indolpyridone that serves as a novel cannabinoid ligand. MN-25 has K_i of 245 nM and 11 nM for CB1 and CB2. MN-25 has CB2 agonist activity and inhibits TNF-R release in human peripheral blood mononuclear cells in vitro with an IC₅₀ of 33 μM. MN-25 shows efficacy in a mouse acute inflammation model at oral doses up to 50 mg/kg^>[1].

L-759656 is a selective cannabinoid CB2 receptor agonist, with the K_i of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin (HY-15371)-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC₅₀ of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.

CB1/2 receptor-1 (compound 5.3) is a CB1/2 receptor agonist. CB1/2 receptor-1 can be used in angiogenesis research.

CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC₅₀ and a K_i of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.

RD-pepcan-11 is a CB1 receptor agonist. RD-pepcan-11 increases the relative phosphorylation level of ERK1/2. RD-pepcan-11 mediates analgesic effects through interaction with CB1 receptors in a carrageenan-induced mouse inflammatory pain model. RD-pepcan-11 can be used in studies related to inflammatory pain.

(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with K_is of both 21 μM.

CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The K_i values for CB2R/FAAH modulator-2 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 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

CB1-receptor agonist-1 is the racemic form of compound ‘1350 and is also a cannabinoid-1 receptor (CB1R) agonist.

R-2 Methanandamide (Compound 2) is a cannabinoid Anandamide (HY-10863) analog with a K_i of 119 nM for the cannabinoid receptor (K_i is determined using rat brain membranes with PMSF).

CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC₅₀ value of 4.2 μM and EC₅₀ value of ＞10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity.

MK-5596 is an efficient, selective and orally active CB1R (IC₅₀ = 1.0 nM, EC₅₀ = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC₅₀ = 3.3 μM, CYP2C8: IC₅₀ = 11 μM, CYP2C9: IC₅₀ = 18 μM, CYP2D6: IC₅₀ = 6 μM). MK-5596 can be used for research on conditions such as obesity.