KARIs, Ghrelin Receptor Agonists With Excellent Brain Permeability, Increase Food Intake and Attenuate the Muscle Loss in Mice - PubMed
19 hours ago
- #Sarcopenia Treatment
- #Brain Permeability
- #Ghrelin Receptor Agonists
- KARIs are novel small-molecule ghrelin receptor (GHSR-1a) agonists with excellent brain permeability.
- KARIs show higher oral bioavailability (63-68%) and brain distribution compared to anamorelin, improving pharmacokinetics.
- In postoperative ileus mice, KARIs activated hypothalamic neurons, increasing food intake and improving gastrointestinal motility.
- In aged mice, KARIs elevated growth hormone levels, restored muscle mass, and enhanced rota-rod performance by modulating muscle-related genes.
- In cancer cachexia models, KARIs preserved muscle mass and improved physical performance at lower doses than anamorelin, without affecting tumor growth.