CB1 Agonist

AM12814 is a potent and partial CB1 and CB2 agonist with K_i values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy.

CB2R/FAAH modulator-1 is a cannabinoid type 2 receptor (CB2R) full agonist with K_is of 14.8 nM and 241.3 nM for CB2R and CB1R, respectively. CB2R/FAAH modulator-1 is a fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ of 4 μM. CB2R/FAAH modulator-1 decreases pro-inflammatory and increases anti-inflammatory cytokines production.

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with K_i values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity.

AM841 is a cannabinoid superagonist and a covalent, irreversible full agonist of CB1. AM841 can activate peripheral CB1 receptors to reduce excitatory neurotransmission and GI smooth muscle contractility, and inhibit synaptic transmission. AM841 is peripherally restricted at low doses in mice, with extremely low brain penetration, potently inhibits gastrointestinal motility, and can reverse acute stress-induced hyperaccelerated gastrointestinal transit; at high doses, it can produce the classic tetrad of central cannabinoid phenotypes (analgesia, catalepsy, hypothermia, decreased spontaneous activity). AM841 can improve intestinal inflammation in mouse colitis models. AM841 induces transient stress-induced hyperthermia. AM841 can be used for research on gastrointestinal motility disorders and colitis.

Δ9-THCB (Δ9-Tetrahydrocannabutol) has a high affinity for human CB1 and CB2 receptors with the K_i values of 15 nM and 51 nM, respectively. Δ9-THCB (Δ9-Tetrahydrocannabutol) has analgesic and anti-inflammatory activities and plays partial agonistic effects on CB1 receptor in mice.

Mead ethanolamide is an endogenous cannabinoid receptor agonist with K_d values of 753 nM and 1810 nM against CB1 and CB2, respectively.

AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 K_i of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity.

RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2.

CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the K_i values of 0.18 μM for CB₁R and 1.22 μM for CB₂R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases.

AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC₅₀ values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms.

PSB-SB1202 (Compound 21a) is a phenyl coumarin compound. PSB-SB1202 is a CB1/CB2 agonist with EC₅₀ values of 56 and 14 nM, and K_i values of 32 and 49 nM, respectively.