GPR119 is expressed in insulin-producing beta cells where it modulates insulin release, thus making it a very attractive therapeutic target for metabolic disorders. GPR119 is activated by oleoylethanolamide (OEA) and by a novel selective small-molecule (PSN632408) which, when administered to high-fat-fed rats, suppresses food intake and reduces body weight gain. Another small molecule full-agonist (AR231453) enhances glucose-dependent insulin release, and improves oral glucose tolerance in wild-type mice, but not in GPR119 knock-out mice.