Lipolysis, the hydrolysis of triglycerides to glycerol and free fatty acids, plays a central role in the regulation of energy balance. In humans, catecholamines are the major lipolytic hormones, upregulating lipolysis via β-adrenoceptors or downregulating lipolysis via α2-adrenoceptors. Exogenous lipolysis regulators are potentially useful in the treatment of obesity, diabetes and cardiovascular disease.














Lipolysis assays are performed in 96– and 384-well format using mature subcutaneous or visceral adipocytes. Isoproternol stimulates fatty acid (NEFA) and glycerol release into the surrounding buffer.