Discovery of 1‐(2,4‐Dichlorophenyl)‐4‐ethyl‐5‐(5‐(2‐(4‐(trifluoromethyl)phenyl)ethynyl)thiophen‐2‐yl)‐<i>N</i>‐(piperidin‐1‐yl)‐1<i>H</i>‐pyrazole‐3‐carboxamide as a Potential Peripheral Cannabinoid‐1 Receptor Inverse Agonist

Abstract

Fast food nation! The title compound (pictured) was identified as a potential peripheral CB1-acting antagonist based on its negative central effects in CB1R agonist-induced hypothermia and analgesia models, and low brain exposure as indicated by the blood-to-plasma ratio. This compound represents a potential lead in the treatment of metabolic disorders.