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Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual CB1 receptor/iNOS inhibitor.Zevaquenabant ((S)-MRI-1867) (3 mg/kg, p.o.) ameliorated obesity-induced kidney morphological and functional changes via decreasing kidney inflammation, fibrosis, oxidative stress, and renal injury.The hybrid CB1R/iNOS inhibitor Zevaquenabant ((S)-MRI-1867) has greater antifibrotic efficacy than inhibition of CB1R alone.(S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diet-induced obesity (DIO mice).
Pregnenolone-d4-1 (3β-Hydroxy-5-pregnen-20-one-d4-1) is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
CB1-IN-1 (BPRCB1184) is a peripherally restricted CB1R antagonist, with Ki of 0.3 nM and 21 nM for CB1R (EC50 = 3 nM) and CB2R, respectively. IC50 value: 0.3 nM (Ki, CB1R) 21 nM (Ki, CB2R) Target: CB1R in vivo: CB1-IN-1 is a novel peripherally restricted cannabinoid 1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice. CB1-IN-1 has great potential to ameliorate this related metabolic syndrome.
AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors; also potent GPR55 agonist (EC50 = 39 nM).