Cannabinoid Receptor Agonist

Anandamide is an endocannabinoid. Anandamide modulates both neuronal and immune functions through two protein-coupled cannabinoid receptors (CB1 and CB2). Anandamide can activate numerous other receptors like PPARS, TRPV1, and GPR18/GPR55. Anandamide also has potential anti-fungal and anti-inflammatory activities. Anandamide can be used for the research of Alzheimer’s disease (AD) and ulcerative colitis.

2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.

Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC₅₀ value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells.

β-Caryophyllene is a CB2 receptor agonist.

ACEA (short for arachidonyl-2'-chloroacetamide) is a synthetic organic compound that acts as an agonist of the cannabinoid receptor CB1. It is a chemical that affects the endocannabinoid system in the body, which regulates various physiological processes such as appetite, pain perception, mood, and memory.

Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .

PSB-KK1415 is a selective agonist for human orphan G protein-coupled receptor GPR18, with EC₅₀ of 19.1 nM.

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB₂) agonist, with an EC₅₀ of 6.2 nM for hCB₂.

Tetrahydromagnolol (Magnolignan), the main metabolite of Magnolol, is a potent and selective cannabinoidCB2 receptor agonist (EC₅₀ =170 nM) and GPR55 antagonist. The K_i of Tetrahydromagnolol for CB2 is 416 nM, 20-fold higher than for the CB1 receptor. Magnolol shows antifungal, anti-inflammatory and analgesic effects.

GW-405833 (L768242) is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values ​​of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i values ​​of 16.1 μM and 4772 nM for CB₁. GW-405833 also exhibits non-competitive CB₁ antagonist, exerting its analgesic and and anti-inflammatory effect through a CB₁ receptor (rather than CB₂) dependent mechanism. GW-405833 can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

β-Caryophyllene (Standard) is the analytical standard of β-Caryophyllene. This product is intended for research and analytical applications. β-Caryophyllene is a CB2 receptor agonist.

CB1 agonist 1 (compound 22) is an agonist of CB1. CB1 agonist 1 shows affinity to CB1 receptor with an pIC₅₀ value of 5.7. CB1 agonist 1 can be used for the research of brain disorders.

PSB-KK1445 is a potent and selective GPR18 agonist with EC₅₀s of 45.4 nM and 124 nM for human and mouse GPR18, respectively. PSB-KK1445 displays >200-fold selectivity versus both CB receptor subtypes, GPR55, and GPR183.

Leelamine hydrochloride is an orally active weakly basic amine that inhibits NPC1 and the androgen receptor AR-V7, and acts as a cannabinoid receptor agonist. Leelamine hydrochloride also functions as a lysosome affinity agent that blocks endocytosis, disrupts autophagic flux and cholesterol transport, thereby altering the RTK-AKT/STAT/MAPK signaling cascade. Leelamine hydrochloride induces cancer cell death and autophagosome accumulation, and can be used in research related to melanoma, castration-resistant prostate cancer and breast cancer.

CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with K_i values of 5.9 nM and 3.5 nM, respectively.

N-Arachidonyldopamine acts as an Anandamide (HY-10863) membrane transport inhibitor, a selective CB₁ cannabinoid receptor agonist, and a VR1 receptor activator. It exhibits an EC₅₀ value of 48 nM for rat VR1 and a K_i value of 0.25 μM for CB1. N-Arachidonyldopamine exists in mammalian neural tissues. It stimulates intracellular Ca²⁺ mobilization, mediates cannabinoid-like effects, and induces hypothermia, hypomotility, catalepsy, analgesia, and hyperalgesia to heat. N-Arachidonyldopamine possesses anticancer activity against breast cancer. It can be used in research related to breast cancer and heat hyperalgesia.

GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC₅₀ values of 63 and 91 nM for human and rat CB2, respectively.

LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB₂) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

GW405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB₂) agonist. GW405833 has EC₅₀ and K_i values ​​of 0.65 nM and 3.92 nM for CB₂, and EC₅₀ and K_i values ​​of 16.1 μM and 4772 nM for CB₁. GW405833 hydrochloride also exhibits non-competitive CB₁ antagonist, exerting its analgesic effect through a CB₁ receptor (rather than CB₂) dependent mechanism. GW405833 hydrochloride can significantly inhibit the production of cAMP stimulated by Forskolin (HY-15371). GW405833 hydrochloride inhibits glycolysis by down-regulating HIF-1α, thereby alleviating acute liver failure (ALF).

MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a K_i of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity.