Cannabinoid Receptor Agonist

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.

β-Caryophyllene-¹³C,d₂ is ¹³C and deuterated labeled β-Caryophyllene (HY-N1415). β-Caryophyllene is a CB2 receptor agonist.

CB2R agonist-5 is a selective CB2R agonist with an EC₅₀ of 48.74 nM. CB2R agonist-5 can be used for the research of pain and immune-related diseases.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist for cannabinoid receptor 2 (CB2 receptor) with an EC₅₀ of 16.2 nM. CB2 receptor agonist 9 inhibits the expression of TNF-α, IL-1β and IL-6, exhibits anti-inflammatory efficacy in DDS (HY-116282)-induced mouse acute colitis model.

(±)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.

O-1269 is a partial agonist of cannabinoid receptor 1 (CB1R) with a K_i of 32 nM. O-1269 shows analgesic effects.

TRPM8 antagonist 4 is a CB2R partial agonist (EC₅₀=54.2 nM, K_i=3.2 μM) and TRPM8 antagonists (IC₅₀=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β.

CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC₅₀s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87.

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.

BPR-890 is a potent agonist of CB1. BPR-890 exhibits excellent CB2/1 selectivity and has in vivo efficacy in diet-induced obese mouse model.

Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC₅₀ values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.

MDA77 is a CB2 inverse agonist with an EC₅₀ of 5.82 nM, showing selectivity for human CB2 and no activity on CB1.

hBChE-IN-2 (compound 15d) is a butyrylcholinesterase (BChE) inhibitor (IC₅₀ of 0.62 μM) and a cannabinoid receptor 2 (CB2R) agonist. hBChE-IN-2 has neuroprotection activities.

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.

APP-FUBINACA is a cannabinoid receptor agonist and a derivative of phenylalaninamide-based indazole-3-carboxamide. APP-FUBINACA exhibits neurostimulatory effects.

CB2R agonist 3 is an agonist of cannabinoid receptor 2 (CB2R), with EC₅₀ of 0.37μM that plays an important role in immune system.

HU 433 is a synthetic cannabinoid CB2 receptor agonist and is the enantiomer of HU 308 (HY-161510). HU 433 exerts its anti-inflammatory and neuroprotective effects by binding to CB2 receptors. HU 433 can be used in the study of neuroinflammation and retinal diseases.

JTE 7-31 selectively acts on peripheral cannabinoid receptors, minimizing central nervous system side effects. They exhibit potent immunomodulatory, anti-inflammatory and anti-allergic properties, as well as inhibitory effects on nephritis.

CB2 receptor agonist 7 (Compound 5B) is a cannabinoid 2 (CB2) receptor agonist with blood-brain barrier permeability.

SMM-189 is  a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research.