cb

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

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 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

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

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

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

EHP-101 (VCE-004.8) is a specific dual agonist of PPARγ and CB2 receptor with potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.

A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in

Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM).

AM251 is a effective CB1 receptor antagonist (IC50/Ki: 8 /7.49 nM) that displays 306-fold selectivity over CB2 receptors; also effective GPR55 agonist (EC50: 39 nM).

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

Org 27569, an allosteric modulator of cannabinoid CB1 receptor, can induce a CB1 receptor state that is characterized by decreased inverse agonist affinity and enhanced agonist affinity.

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

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

Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.

Yangonin (Y100550) is a novel CB receptor ligand, it exhibits affinity for the human recombinant CB receptor. Yangonin (Y100550) could be a valuable candidate for the intervention of NF-κB-dependent pathological conditions such as inflammation.

JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.

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.

(±)-Ibipinabant ((±)-SLV319) has been utilized in clinical trials for the treatment of obesity and type 2 diabetes.

BML-190 (Indomethacin morpholinylamide) is a specific CB2 receptor inverse agonist (Ki: 435 nM), with 50-fold selectivity over CB1 receptor.

GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.

LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively).