Differential tissue distribution of the enantiomers of racemic pindolol in the rat.
Racemic pindolol, a beta-adrenoceptor and a 5-HT1A/1B receptor antagonist, has been reported to augment and accelerate the clinical efficacy of antidepressants. The (S)-enantiomer is more potent than the (R)-enantiomer both at the beta-adrenergic and at the 5-HT1A/1B receptors. A chiral HPLC column was used for determination of tissue concentrations of the enantiomers of pindolol at 90 min after 8 mg/kg s.c. of the racemate. The (S)/(R) ratio was found to vary between tissues from 1.74 in brain to 0.82 in plasma. The present findings may be important for understanding the pharmacodynamic actions of racemic pindolol.
Yan
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H
Department of Neuroscience, Psychiatry, Ulleråker, Uppsala University, Sweden. hongmei.yan@ullpsyk.uu.se
Lewander
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T
D000273:Adipose Tissue / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D009132:Muscles / Q000378:metabolism; D009206:Myocardium / Q000378:metabolism; D010869:Pindolol / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012702:Serotonin Antagonists / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D013154:Spleen / Q000378:metabolism; D013237:Stereoisomerism; D014018:Tissue Distribution
D012702:Serotonin Antagonists; D010869:Pindolol