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Open Access Gold as soon as Publ. Version/Full Text is submitted to ZB.
Ecotoxicology of narcosis: Stereoselectivity and potential target sites.
Chemosphere 72, 1256-1259 (2008)
The stereoselectivity of certain anesthetics is currently thought to be inconsistent with lipid theories of narcosis. The EC(50)-values of etomidate enantiomers for tadpole narcosis are now examined as a function of octanol/water partition coefficients, and enhancement factors for predicted over experimental EC(50) values are determined from a calibration curve for non-selective narcosis. The unfavored S-(-)-enantiomers of etomidate and two analogues surprisingly still fulfill the Meyer-Overton rule. The R(+)-enantiomers of etomidate and four structural analogues are up to 34-fold more active than expected. The non-chiral anesthetic, propofol, is 8-fold more active than expected. It is concluded that there may be two pathways to tadpole narcosis: enhanced narcosis involving specific receptor binding sites and non-selective narcosis corresponding to the Meyer-Overton rule and operating on the lipid/protein interface.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Tadpole narcosis; Stereoselectivity; Etomidate; Propofol; GABAA channel; Lipid/protein interface
ISSN (print) / ISBN
0045-6535
e-ISSN
1879-1298
Journal
Chemosphere
Quellenangaben
Volume: 72,
Issue: 9,
Pages: 1256-1259
Publisher
Elsevier
Publishing Place
Kidlington, Oxford
Reviewing status
Peer reviewed
Institute(s)
Institute of Biochemical Plant Pathology (BIOP)