8-Chlorotheophylline

**8-Chlorotheophylline** is a stimulant drug of the xanthine chemical class with physiological effects similar to caffeine. Its primary use is as a component of the antiemetic drug dimenhydrinate (marketed as Dramamine and Gravol), where it is combined in a salt form with diphenhydramine. The stimulant properties of 8-chlorotheophylline are intended to counteract the drowsiness caused by diphenhydramine’s antihistaminic activity in the central nervous system. Mechanistically, its effects are mainly attributed to antagonism at adenosine receptors (notably A2a), leading to increased neuronal excitation. While classified as a xanthine stimulant like caffeine or theophylline, it does not cross the blood-brain barrier well and generally does not produce significant locomotor stimulation in animal models[1][2][3][5].

Other names

chlorotheophylline1,3-dimethyl-8-chloroxanthine8-chloro-1,3-dimethylpurinedione