Peripherally Restricted, Highly Potent, Selective, Aqueous-Soluble EP2 Antagonist with Anti-Inflammatory Properties.
Sign Up to like & getrecommendations! Published in 2018 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.8b00764
Abstract: The prostaglandin E2 receptor, EP2, plays an important role in physiology and in a variety of pathological conditions. Studies indicate that EP2 is pro-inflammatory in chronic peripheral and central nervous system disease and cancer models.… read more here.
Keywords: anti inflammatory; peripherally restricted; restricted highly; inflammatory ... See more keywords
Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB1R Inverse Agonists.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00495
Abstract: The 6-benzhydryl-4-amino-quinolin-2-ones are peripherally restricted CB1 receptor inverse agonists (CB1RIAs) that have been reported to attenuate obesity and improve insulin sensitivity in the diet-induced obese (DIO) mouse model. However, chronic dosing of select compounds from… read more here.
Keywords: peripherally restricted; inverse agonists; benzhydryl amino;
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00406
Abstract: The effects of opioids in the central nervous system (CNS) provide significant benefit in the treatment of pain but can also lead to physical dependence and addiction, which has contributed to a growing opioid epidemic… read more here.
Keywords: receptor antagonist; peripherally restricted; opioid receptor; restricted opioid ... See more keywords