التفاصيل البيبلوغرافية
| العنوان: |
Stereoselective Potencies and Relative Toxicities of Coniine Enantiomers. |
| المؤلفون: |
Stephen T. Lee, Benedict T. Green, Kevin D. Welch, James A. Pfister, Kip E. Panter |
| المصدر: |
Chemical Research in Toxicology. Sep2008, Vol. 21 Issue 10, p2061-2064. 4p. |
| مصطلحات موضوعية: |
*ENANTIOMERS, *OPTICAL isomers, *CHIRALITY, *CHIRAL drugs |
| مستخلص: |
Coniine, one of the major toxic alkaloids present in poison hemlock ( Conium maculatum), occurs in two optically active forms. A comparison of the relative potencies of (+)- and (−)-coniine enantiomers has not been previously reported. In this study, we separated the enantiomers of coniine and determined the biological activity of each enantiomer in vitroand in vivo. The relative potencies of these enantiomers on TE-671 cells expressing human fetal nicotinic neuromuscular receptors had the rank order of (−)-coniine > (±)-coniine > (+)-coniine. A mouse bioassay was used to determine the relative lethalities of (−)-, (±)-, and (+)-coniine in vivo. The LD 50values of the coniine enantiomers were 7.0, 7.7, and 12.1 mg/kg for the (−)-, (±)-, and (+)- forms of coniine, respectively. The results from this study demonstrate that there is a stereoselective difference in the in vitropotencies of the enantiomers of coniine that directly correlates with the relative toxicities of the enantiomers in vivo. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
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