Cannabinoid Receptor Modulator

Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.

ZCZ011 is a potent and brain-penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain.

CB1R Allosteric modulator 5 (compound 3) is a selective, and blood-brain barrier (BBB) permeable Cannabinoid receptor type 1 allosteric modulator with a pIC₅₀ of 6.89. CB1R Allosteric modulator 5 attenuates both cocaine-seeking behavior specific to cue-induced reinstatement and cocaine-induced behavioral sensitization without altering locomotor activity.

PSB-SB-487 is a potent GPR55 antagonist and CB₂ agonist with an IC₅₀ value of 0.113 µM for GPR55, and a K_i value of 0.292 µM for human CB₂. PSB-SB-487 can be used for researching diabetes, Parkinson’s disease, neuropathic pain, and cancer.

CB2 modulator 1 (compound 130) is a potent CB2 modulator. CB2 modulator 1 has the potential for immunedisorders, inflammation, osteoporosis, renal ischemia.

(R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor mediators for research of obesity and metabolic disease

GAT229 is a CB1 positive allosteric modulator (PAM) that effectively reduces intraocular pressure (IOP) in high IOP mouse models and enhances CB1 receptor-mediated IOP-lowering effects. A 0.2% GAT229 solution or 10 mg/kg of GAT229 alone significantly reduces IOP. GAT229 is promising for research related to glaucoma and elevated intraocular pressure.

Virodhamine TFA is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine TFA induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine TFA can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases.

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB₁) receptor with a pIC₅₀ of 7.54 in Ca²⁺ mobilization assay. RTICBM-189 has pIC₅₀s of 5.29 and 6.25 for hCB₁ and mCB₁, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats.

CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.

CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC₅₀ values of 0.018 μM and 1.241 μM, respectively.

PSB-SB-1203 (Compound 25b) is a dual CB1/CB2 ligand that blocks CB1 but activates CB2 receptors (CB1 K_i 0.244 μM; CB2 K_i 0.210 μM, EC₅₀ 0.054 μM). PSB-SB-1203 is promising for research of obesity and cancers.

Dodec-2E-ene-8,10-diynoic acid isobutylamide is an alkamide found in Echinacea angustifolia that binds to CB₁ (rat K_i = 61.1 μM) and CB₂ (mouse K_i = 47.2 μM) cannabinoid receptors. Dodec-2E-ene-8,10-diynoic acid isobutylamide can be used in research on inflammatory diseases.

MDA-19 N-(5-hydroxyhexyl) is a cannabinoid receptor modulator targeting CB1R/CB2R. MDA-19 N-(5-hydroxyhexyl) is used to study neurological diseases, cancer, and pain regulation.

GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases.

RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC₅₀ values of 23 nM (calcium mobilization assay) and 153 nM ([³⁵S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder.

CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC₅₀s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.

CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC₅₀  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.