Mechanism of action: Melanin concentrating hormone receptor 1 (MCH1) antagonist

Preclinical pharmacology

AZ13483342 is an antagonist at the MCH1 receptor with a potency of 8.6nM (IC50). Potency in rats and mice corresponds well to the potency at the human receptor. Receptor occupancy in vivo in mice gives an unbound IC50 potency of 2nM in plasma. The compound showed no efflux in Caco2 cells and a 1:1 ratio of unbound concentration in brain to plasma has been measured in PET experiments in Rhesus monkeys demonstrating good CNS exposure is achieved in vivo.

In Dietary Induced Obese (DIO) mice, the compound is well tolerated and reduces body weight by reduction of body fat mass in studies over 21 days.

Additional Information

Gene information from the NCBi

This compound works on the following genes: