Our understanding of biliary motility under normal and pathophysiologic conditions is still incomplete, but there have been recent advances. Of particular interest are the mechanisms involved in gallbladder filling and emptying, with a focus on understanding the processes underlying impaired gallbladder emptying leading to gallbladder dyskinesia and the formation of gallstones or cholecystitis. The sphincter of Oddi (SO) is a complex neuromuscular structure. Recent studies have attempted to unravel the specific neural or hormonal mechanisms operating under normal physiologic conditions and those that may lead to SO dysfunction. Furthermore, new research fronts are emerging, including the role of leptin in obese patients with impaired biliary motility and the action of electroacupuncture for possible treatment of SO dysfunction. This review illustrates the broad front of current research regarding the effects of bioactive agents on biliary motility, including enteric hormones, nitric oxide, opioids, inflammatory mediators, leptin, protease inhibitors, neurotransmitters, and electroacupuncture.