Cannabinoid Receptor Agonist

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC₅₀ of 8 for hCB2, and a pK_i of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors.

S-1 Methanandamide ((S)-Methanandamide), an Anandamide analog, is a CB1 receptor ligand with a K_i of 173 nM. S-1 Methanandamide inhibits electrically-evoked twitch response in mouse vas deferens with an IC₅₀ value of 230 nM.

CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a K_i of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

Arachidonoyl ethanolamide phosphate, an endocannabinoid, is an endogenous ligand for cannabinoid receptors in the central nervous system (CB1 subtype) and peripheral immune cells (CB2 subtype).

L759633 is a potent and selective agonist of cannabinoid receptor (CB₂) receptor, with K_is of 6.4 nM and 1043 nM for CB2 and CB1 receptors, respectively. L759633 can inhibit Forskolin-stimulated cAMP production.

RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca²⁺ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (K_i=50 nM).

Bay 59-3074 is a selective cannabinoid CB₁/CB₂ receptor partial agonist with K_i values of 48.3 and 45.5 nM at human CB₁ and CB₂ receptors, respectively. Bay 59-3074 has analgesic properties.

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.

OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC₅₀=75 nM) and cannabinoid receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM.

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.

Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.

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.

Vicasinabin (RG7774) is an orally active, selective, and full CB2R agonist, with EC₅₀ values of 2.81 nM and 2.60 nM for human CB2R and mouse CB2R, respectively. Vicasinabin inhibits inflammation, reduces leukocyte adhesion and decreases vascular permeability by selectively activating CB2R. Vicasinabin can be used in the researches for diabetic retinopathy, uveitis and laser-induced choroidal neovascularization.

CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with K_is of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.

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.

S-777469 is a selective and orally available cannabinoid type 2 receptor (CB2) agonist with a K_i of 36 nM. S-777469 significantly suppresses compound 48/80-induced scratching behavior in mice in a dose-dependent manner. S-777469 produces its antipruritic effects by inhibiting itch signal transmission through CB2 agonism.

GP1a is a potent agonist of cannabinoid receptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization.

β-Caryophyllene-d₂ is deuterium labeled β-Caryophyllene. β-Caryophyllene is a CB2 receptor agonist.

Eicosapentaenoyl ethanolamide-d₄ is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant.

SER-601 is a potent and selective peripheral cannabinoid (CB2) receptor agonist with a K_i of 6.3 nM. SER-601 has analgesic and antidiabetic properties and can be used for relevant research.