ENP11, a potential CB1R antagonist, induces anorexia in rats.

摘要: Abstract Over the past decade, pharmacological manipulation of cannabinoid 1 receptor (CB1R) has become an interesting approach for management food ingestion disorders, among other physiological functions. Searching new substances with similar desirable effects, but fewer side-effects we have synthesized a SR141716A (a inverse agonist also called Rimonabant) analog, 1-(2,4-Difluorophenyl)-4-methyl-N-(1-piperidinyl)-5-[4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carboxamide, ENP11, that so far, as previously shown, induced changes in glucose availability, i.e. hypoglycemia, rats. In this study tested if any, ENP11 (0.5, 1.0, and 3.0 mg/kg) ingestion, core temperature, pain perception motor control adult Wistar Results showed reduced during first hour immediately after administration. Likewise, (1.0 mg/kg) blocked anandamide (AEA)-induced hyperphagia 4 h dark phase light–dark cycle, it AEA-induced hypothermia. However, none doses used affected or control. We believe is potential useful CB1R antagonist reduces regulates temperature.