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Zevaquenabant
Zevaquenabant (S-MRI-1867, INV-101, or MRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at the National Institutes of Health. Zevaquenabant was described as a third generation cannabinoid receptor 1 (CB1R) antagonist due to its peripheral selectivity and polypharmacology. It acts as a peripherally selective inverse agonist of the cannabinoid receptor 1 and an inducible nitric oxide synthase (iNOS) inhibitor. It has been studied in the experimental models of fibrotic disorders such as liver fibrosis /sup>, chronic kidney disease, idiopathic pulmonary fibrosis, Hermansky-Pudlak syndrome pulmonary fibrosis, skin fibrosis, and metabolic disorders such as obesity /sup> and dyslipidemia Dyslipidemia is a metabolic disorder characterized by abnormally high or low amounts of any or all lipids (e.g. fats, triglycerides, cholesterol, phospholipids) or lipoproteins in the blood. Dyslipidemia is a risk factor for th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Monlunabant
Monlunabant (INV-202, MRI-1891, or S-MRI-1891) is a peripherally selective cannabinoid receptor 1 inverse agonist, discovered as a β-arrestin-2-biased cannabinoid receptor 1 antagonist by Dr George Kunos, Dr Resat Cinar, and Dr Malliga Iyer at the National Institutes of Health. It was developed as a weight loss drug by Inversago Pharma. Novo Nordisk’s obesity drug monlunabant showed only modest weight loss in a Phase 2a trial. The drug was associated with higher rates of mild to moderate neuropsychiatric side effects like anxiety and sleep disturbances. Suicidal ideations were not reported. See also * Zevaquenabant Zevaquenabant (S-MRI-1867, INV-101, or MRI-1867) is an investigational small-molecule drug, discovered by Dr George Kunos, Dr Resat Cinar, and Dr Malliga iyer at the National Institutes of Health. Zevaquenabant was described as a third generation ... References {{Cannabinoid receptor modulators CB1 receptor antagonists Experimental anti-obesity drugs Peri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripheral Selectivity
Peripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation. These peripherally selective opioids can be used as antidiarrheals, for instance loperamide (Imodium). Mechanisms of peripheral selectivity include physicochemical hydrophilicity and large molecular size, which prevent drug permeation through the lipid bilayer cell membranes of the blood–brain barrier, and efflux out of the brain by blood–brain barrier transporters such as P-glycoprotein among many others. Transport out of the bra ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |