The aim of this study was to evaluate the lipolytic potential of solutions used in the practice of cosmetic mesotherapy to stimulate lipolysis, cause local fat reduction and reduce the appearance of cellulite. The mesotherapy solutions were tested in a human fat cell assay using the fold induction of glycerol generation as a measure of lipolysis. The following mesotherapy solutions were tested: aminophylline; yohimbine; isoproterenol; melilotus; aminophylline with melilotus; aminophylline with isoproterenol; aminophylline with isoproterenol and yohimbine; aminophylline with isoproterenol and lidocaine; and aminophylline with isoproterenol, yohimbine and lidocaine. Isoproterenol (P<0.002), aminophylline (P<0.00004) and yohimbine (P<0.001) stimulated lipolysis compared to the buffer control. The lipolysis stimulated by melilotus (P<0.01) and isoproterenol (P<0.002) was enhanced by aminophylline (P<0.001 and P<0.001, respectively). The lipolytic stimulation by aminophylline and isoproterenol (P<0.0009), and by aminophylline and isoproterenol with yohimbine (P<0.0007) was inhibited by lidocaine, not significant compared to buffer control for aminophylline and isoproterenol, but aminophylline, isoproterenol and yohimbine still stimulated lipolysis more than control, P<0.05). Isoproterenol, aminophylline, yohimbine and melilotus stimulate lipolysis alone, and lipolysis is further enhanced by combining lipolytic stimulators in mesotherapy solutions. Lidocaine is antilipolytic and should be removed from mesotherapy solutions designed for local fat reduction.