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The purpose of this study was to further investigate the differences in the effects of optical isomers of chlorpheniramine (d-, l- and dl-forms) on the levels of dopamine (DA) and 3,4-dihydroxyphenylacetic acid (DOPAC) in the regional parts of rat brain. After the intravenous administration of each form of chlorpheniramine at a dose of 20 mg/kg, the DA and DOPAC levels were measured by HPLC system. Each form of chlorpheniramine is effective in reducing DOPAC, but not DA levels in the brain of rats. The degree of reducing DOPAC levels does not correlate with the antihistaminic potency of these drugs. Thus, the present results indicate that there is a lack of stereospecificity in reducing DOPAC levels, suggesting the lack of stereospecificity in inhibiting DA reuptake.

Effects of d-, l- and dl-Chlorpheniramine on Dopamine and 3,4-Dihydroxyphenylacetic Acid Levels in the Regional Parts of Rat Brain.