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 The National Institutes of Health (NIH) is the primary agency of the United States government responsible for biomedical and public health research. It was founded in 1887 and is part of the United States Department of Health and Human Service ...

. Zevaquenabant was described as a third generation

cannabinoid receptor 1 Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the ''CNR1'' gene. And discovered, by determination and characterization in 1988, and cloned in 1990 for the first time. The human CB1 recep ...

(CB1R) antagonist due to its peripheral selectivity and

polypharmacology Polypharmacology is the design or use of pharmaceutical agents that act on multiple targets or disease pathways. Despite scientific advancements and an increase of global R&D spending, drugs are frequently withdrawn from markets. This is primarily ...

. It acts as a peripherally selective

inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agon ...

of the

and an inducible nitric oxide synthase (iNOS) inhibitor. It has been studied in the experimental models of fibrotic disorders such as

liver fibrosis Cirrhosis, also known as liver cirrhosis or hepatic cirrhosis, chronic liver failure or chronic hepatic failure and end-stage liver disease, is a chronic condition of the liver in which the normal functioning tissue, or parenchyma, is replaced ...

^{/sup>, chronic kidney disease

Chronic kidney disease (CKD) is a type of long-term kidney disease, defined by the sustained presence of abnormal kidney function and/or abnormal kidney structure. To meet criteria for CKD, the abnormalities must be present for at least three mo ...
, idiopathic pulmonary fibrosis

Idiopathic pulmonary fibrosis (IPF) synonymous with cryptogenic fibrosing alveolitis is a rare, progressive illness of the respiratory system, characterized by the thickening and stiffening of lung tissue, associated with the formation of scar ...
, Hermansky-Pudlak syndrome pulmonary fibrosis, skin fibrosis, and metabolic disorders such as obesity

Obesity is a medical condition, considered by multiple organizations to be a disease, in which excess Adipose tissue, body fat has accumulated to such an extent that it can potentially have negative effects on health. People are classifi ...
^{/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 the development of ...
.

See also

* Monlunabant

References

{{Cannabinoid receptor modulators

CB1 receptor antagonists
Enzyme inhibitors
Experimental drugs
Small-molecule drugs
4-Chlorophenyl compounds
Pyrazolines
Guanidines
Sulfonamides
Peripherally selective drugs}}