Cannabinoid Receptor Inhibitor

RTICBM-303 is a blood-brain barrier-penetrant cannabinoid receptor type 1 (CB₁) inhibitor. RTICBM-303 concentration-dependently decreases the E_max of the agonist CP55,940, increases the binding of [³H]CP55,940, and inhibits CB₁ receptor signaling. RTICBM-303 selectively reduces cue-induced and drug-priming-induced drug-seeking relapse behaviors in rats. RTICBM-303 can be used in studies related to addictive behaviors.

TC-C 14G (Compd 14g) is a Cannabinoid-1 Receptor (CB1R) inverse agonist, with a K_i of 4 nM and EC₅₀ of 11 nM for HCB1R, respectively.

UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase.

N-(3-Hydroxyphenyl)-arachidonoyl amide (Compound 23) is an anandamide transport inhibitor with an IC₅₀ of 21.3 μM.

UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide.

O-Arachidonoyl glycidol (compound 1) is a 2-arachidonoylglycerol (2-AG) analog. O-Arachidonoyl glycidol inhibits cytosolic 2-oleoylglycerol (2-OG) hydrolysis with an IC₅₀ value of 4.5 µM. O-Arachidonoyl glycidol blocks 2-OG hydrolysis in membrane fractions and anandamide hydrolysis with IC₅₀s of 19, 12 µM, respectively.

Pregnenolone monosulfate (sodium)-¹³C₂,d₂ is the ¹³C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

CB1-IN-2 (Compound 4g) is a selective CB₁ inhibitor with an IC₅₀ of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant.

SGC stimulator 2 is an orally active soluble guanylyl cyclase (sGC) stimulator with an EC₅₀ of 44 nM. SGC stimulator 2 exhibits inhibitory activity against the CB₂ receptor, with an IC₅₀ of 2.7 μM. SGC stimulator 2 activates native (Fe²⁺) sGC in a heme-dependent manner. SGC stimulator 2 produces sustained hypotensive effects in animal models. SGC stimulator 2 can be used for the research of hypertension.

CB1-IN-3 (Compound 6i) is a potent cannabinoid type 1 receptor (CB1) inhibitor. CB1-IN-3 is promising for research of obesity, inflammation, and neurological diseases.

Yangonin (Standard) is the analytical standard of Yangonin. This product is intended for research and analytical applications. Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.

Palmitoylisopropylamide is a Palmitoylethanolamide analogue inhibits [³H]-Anandamide metabolism with a pI₅₀ of 4.89.

Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.

Taranabant ((1R,2R)stereoisomer) (Standard) is the analytical standard of Taranabant ((1R,2R)stereoisomer) (HY-10013B). This product is intended for research and analytical applications. Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.

Pregnenolone monosulfate (sodium) (Standard) is the analytical standard of Pregnenolone monosulfate (sodium). This product is intended for research and analytical applications. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication. Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

CH-PIATA is a synthetic cannabinoid with an acetamide linker. CH-PIATA can be detected as parent substance in blood samples. CH-PIATA has EC₅₀ values of >71 and >176 nM for CB₁ and CB₂, respectively.

RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC₅₀ = 8.7 nM) and shows high binding affinity for rat DAT with a K_i value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.

MRL-650 (CB1 inverse agonist 1), a chemical probe, is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC₅₀s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects.