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Selected Publication:
Stoschitzky, K; Lindner, W; Kiowski, W.
Stereoselective vascular effects of the (R)- and (S)-enantiomers of propranolol and atenolol.
J Cardiovasc Pharmacol. 1995; 25(2):268-272
Doi: 10.1097/00005344-199502000-00012
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- Leading authors Med Uni Graz
- Stoschitzky Kurt
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- Abstract:
- All beta-adrenergic antagonists have an asymmetric carbon atom, and most commercially available beta-blockers consist of (R)- and (S)-enantiomers in a fixed 1:1-ratio. The drugs are believed to be contraindicated when peripheral vascular disease exists, presumably due to unopposed alpha-adrenergic vasoconstriction. However, little is known about direct vascular effects of beta-blockers or of stereoselective effects on peripheral arteries. Therefore, we investigated the effects on forearm blood flow (FBF) of brachial artery infusions of the (R)- and (S)- enantiomers of propranolol and atenolol (2, 10, and 50 micrograms/min each) and their inhibitory effects on isoprenaline (Iso)-induced vasodilatation by forearm venous occlusion plethysmography in 12 healthy subjects. Only (R)-propranolol caused an increase in FBF (+21%, p < 0.05), whereas (S)-propranolol and (R)- and (S)-atenolol had no direct effect on peripheral arteries. Vasodilatation induced by Iso was abolished by (S)-propranolol and reduced by (R)-propranolol (-56%, p < 0.05) and (S)-atenolol (-68%, p < 0.05), whereas (R)-atenolol had no effect. Our results indicate that the optically pure (R)- and (S)-enantiomers of propranolol and atenolol do not exert direct vasoconstrictive effects. Furthermore, our results confirm that predominantly (S)-enantiomers have beta-adrenoceptor blocking effects, but they also show that neither the non-beta-blocking (R)-enantiomer of propranolol nor the (S)-enantiomer of the beta 1-selective agent atenolol is completely devoid of blocking effects on vascular beta 2-adrenoceptors.
- Find related publications in this database (using NLM MeSH Indexing)
- Adult -
- Analysis of Variance -
- Atenolol - pharmacology
- Blood Pressure - drug effects
- Forearm - blood supply
- Humans - blood supply
- Male - blood supply
- Plethysmography - blood supply
- Propranolol - pharmacology
- Regional Blood Flow - drug effects
- Stereoisomerism - drug effects
- Structure-Activity Relationship - drug effects
- Vascular Resistance - drug effects
- Vasoconstriction - drug effects
- Vasodilation - drug effects
- Find related publications in this database (Keywords)
- Propranolol
- Atenolol
- Beta-Blockers
- Stereoselectivity
- Forearm Blood Flow