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

Abstract

of d-, land dl-Chlorpheniramine on Dopamine and 3, 4-Dihydroxyphenylacetic Acid Levels in the Regional Parts of Rat Brain. Tohoku J. Exp. Med., 1991, 163 (4), 239-244 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.chlorpheniramine ; dopamine ; 3, 4-dihydroxyphenylacetic acid ; histamine H1-blocker

Chlorpheniramine exerts anxiolytic-like effects and activates prefrontal 5-HT systems in mice

“…Therefore, the chlorpheniramine-induced increase of extracellular 5-HT levels unlikely results from a blockade of histamine H 1 receptors. Previous reports indicated that chlorpheniramine blocks 5-HT reuptake (Lidbrink et al 1971;Sakurai et al 1991;Shishido et al 1991;Young et al 1988), in keeping with its high binding affinity for 5-HT transporters (Kd= 5.2±0.8 nM, according to Tatsumi et al 1997). Since it is unknown whether chlorpheniramine facilitates 5-HT release, chlorpheniramine likely increases extracellular 5-HT levels via the inhibition of 5-HT reuptake.…”

Quantitative radioluminography of serotonin uptake sites in the porcine brain

“…trations are similar in brain of swine (Prelusky et al, 1991) and rodent (Dewar et al, 1991;Sakurai et al, 1991;Shoaf et al, 2000). Some serotonin concentrations measured in extracts from swine brain were nil in cerebellum, 50 ng/gram in hippocampus, and 250 ng/g in hypothalamus (Prelusky et al, 1991).…”