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Three-dimensional view of pharmacology.
Am J Hosp Pharm
September 1992
Department of Oncology, McGill University, Montreal, Quebec, Canada.
The relationship between the stereochemistry of drugs and their therapeutic and toxic effects is discussed. Molecular structures that have the same chemical constituents and are related to each other as an object and its nonsuperimposable mirror image are enantiomers. A molecule that has at least one pair of enantiomers is a chiral compound, and a 50:50 mixture of enantiomers is a racemic mixture.
View Article and Find Full Text PDFBinding of dextromethorphan (DM) to guinea pig brain is stereoselective, since levomethorphan is 20 times weaker than DM in competing for DM sites. In general, opiate agonists and antagonists as well as their corresponding dextrorotatory isomers are weak competitors for tritiated dextromethorphan ([3H]DM) binding sites and display IC50 values in the micromolar range. In contrast, several non-narcotic, centrally acting antitussives are inhibitory in the nanomolar range (IC50 values for caramiphen, carbetapentane, dimethoxanate, and pipazethate are 25 nM, 9 nM, 41 nM, and 190 nM, respectively).
View Article and Find Full Text PDF1. When l-propoxyphene-N-oxide was given orally to dogs, reduction occurred in vivo resulting in substantial plasma levels of l-propoxyphene. 2.
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