Receptor de cannabinoides

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).

A-836339: Potent cannabinoid, CB2-focused (Ki=0.64nM), lesser CB1 affinity (Ki=270nM); analgesic, anti-inflammatory in mice.

CB2R agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [

N-Arachidonyldopamine (NADA) is a selective and potent endogenous CB1 receptor agonist (Ki: 250 nM).N-Arachidonyldopamine is also a potent and selective TRPV1

BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体,其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

Δ8-THC-C8 is a semi-synthetic cannabinoid. It acts as an agonist for the cannabinoid receptor 1 (CB1) with an EC50 value of 13.8 nM.

AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2R/FAAH modulator-1: agonizes CB2R, inhibits FAAH (IC50=4 μM), alters cytokine production; used in inflammation research. Ki: CB2R=14.8 nM, CB1R=241.3 nM.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

Evofolin B is a natural compound isolated from the stem bark of Zanthoxylum ailanthoides.

JHU 75528 (JHU-75528) is a novel PET tracer with inhibitory effects on CB that can be used to study the cannabinoid system in schizophrenic patients.

CB2R/FAAH modulator-3 (compound 27) is a modulator targeting at CB2R and FAAH.

AM251: potent CB1 blocker (IC50: 8 nM), 306x CB2 selective; GPR55 activator (EC50: 39 nM).

Pregnenolone acetate inhibits CB1 receptors, blocking THC effects and shielding the brain from cannabis intoxication.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1.

GW 833972A: selective CB2 agonist; reduces neural depolarization and citric acid cough in animals.

ML-193: GPR55 antagonist, IC50 221nM, 27x selective over GPR35/CB1/CB2, may aid Parkinson's symptoms.

AM-2232 (UNII-40KCH8YIKP) is a potent and unselective agonist of the cannabinoid receptors.

(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].

Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].

Delta8-THC acetate (Delta8-tetrahydrocannabinol) is a psychoactive cannabinoid that binds to the cannabinoid receptor 1 (CB1 receptor) and exhibits anti-nausea, appetite-stimulating, and anti-inflammatory effects. It may also offer neuroprotective benefits and has potential applications in research on anxiety and depression.

2'-Hydroxydaidzein is an isoflavonoid phytonutrient found in plant species, when a natural compound. 2'-Hydroxydaidzein has antioxidant activity, driven mainly by o-hydrogen bond dissociation enthalpy (BDE) and hydrogen atom transfer (HAT) mechanisms. 2'-Hydroxydaidzein inhibits chemical mediators in inflammatory cells and may be of value in the treatment and prevention of inflammatory diseases associated with excessive chemical mediator production. It may have a role in the treatment and prevention of central and peripheral inflammatory diseases associated with excessive chemical mediator production. 2'-Hydroxydaidzein inhibited the release of neutrophils and formyl-Met-Leu-Phe/cytochalasin B (fMLP/CB) in rats, with IC(50) values of 2.8+/-0.1 and 5.9+/-1.4 microM, respectively.

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

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.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM).

CB2R PAM, an oral drug, boosts CB2 receptor response to specific agonists, showing potential in neuropathic pain relief.

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R.

CB2 receptor agonist 2 (ZINC72105556): potent, Ki=8.5 nM, high selectivity for CB2.

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH.

Olivetol, found in lichens, is an organic antioxidant and THC synthesis precursor.

ML192 (CID1434953) is a selective GPR55 ligand antagonist.

(±)-Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the TRPA1.

ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with EC50 of 0.26 μM.

SCH-336: potent, selective CB2 agonist (Ki=1.8 nM, EC50=2 nM), orally active, 100x CB2 vs. CB1 preference, reduces leukocyte migration and eosinophilia.

EHP-101 is a PPARγ/CB2 dual agonist with anti-inflammatory properties, inhibits fat formation, and combats diet-related obesity.

Pregnenolone (Arthenolone) is an endogenous steroid hormone synthesized from cholesterol, used in the treatment of Alzheimer's disease.

Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

CB1/2 agonist 3 is a competitive and potent CB1/CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.

Pregnenolone monosulfate sodium salt is an neurosteroid, enhances NMDA receptor,CREB phosphorylation, TRPM3 channels, and may inhibit GABA A receptors.

Noladin ether (2-AG ether) is a cannabinoid CB1 receptor agonist.

Otenabant (CP-945598) has been investigated for the treatment of Obesity.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.

(±)-Ibipinabant ((±)-SLV319) has been used in trials studying the treatment of Obesity and Obesity and Type 2 Diabetes.

Olorinab (APD 371) (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.

BAY 38-7271: potent neuroprotective, selective CB1/CB2 agonist, Ki of 1.85 nM (CB1) & 5.96 nM (CB2).