Cannabinoid 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.

GW 833972A free base is a selective CB₂ receptor agonist with pEC₅₀ of the human CB₂ receptor for GW 833972A free base of 7.3, and its selectivity for the CB₂ receptor is approximately 1000 times higher than that for the CB₁ receptor. GW 833972A free base inhibits induced neuronal depolarization and suppresses coughing caused by citric acid in guinea pig models. GW 833972A free base can be used for the study of chronic cough.

CB2 receptor agonist 4 (Compound 8) is a highly selective cannabinoid receptor type 2 (CB2 Receptor) agonist with an EC₅₀ of 13.99 nM. CB2 receptor agonist 4 shows no significant activity against cannabinoid receptor type 1. CB2 receptor agonist 4 can be used for the research of pain and immune-related diseases.

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.

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.

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.

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.

Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC₅₀=2 nM).

2-Arachidonoylglycerol-d₈ is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.

Anandamide-d8 is a deuterated labeled Anandamide. 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.

VSN-16 is a cannabinoid receptor agonist with vasodilatory activity. VSN-16 can be used for the study of multiple sclerosis.

BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively).

CB65 is a potent and high affinity CB2 selective agonist with a K_i value of 3.3 nM. CB65 exhibits a K_i of >1000 nM for CB1 receptor.

2-Arachidonoylglycerol-d₅ is the deuterium labeled 2-Arachidonoylglycerol. 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system.

A-836339 is a selective CB2 receptor agonist, with Ki values of 0.4 nM and 0.8 nM in humans and rats, respectively. A-836339 exhibits multiple effects such as analgesia, gastric protection, anti-inflammation, and antioxidant activity. A-836339 produces antinociceptive and analgesic activities by activating CB2 receptors in the dorsal root ganglia and spinal cord. A-836339 can also exert gastric protective effects through anti-inflammatory mechanisms (reducing TNF-α and IL-1β) and antioxidant mechanisms (enhancing the activities of CAT and SOD, and reducing H₂O₂). Radioactively labeled A-836339 can serve as a CB2-specific radioligand for autoradiography and PET imaging. A-836339 can be used in research on inflammatory pain, neuropathic pain, gastric ulcers, cerebral ischemia, etc.

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.